1、 HYPERLINK https:/www.MedChemE/Targets/Glucocorticoid Receptor.html Glucocorticoid HYPERLINK https:/www.MedChemE/Targets/Glucocorticoid Receptor.html HYPERLINK https:/www.MedChemE/Targets/Glucocorticoid Receptor.html ReceptorGlucocorticoid Receptor (GR, or GCR) also known as NR3C1 (nuclear receptor

2、subfamily 3, group C, member 1) is the receptor towhich cortisol and other glucocorticoids bind. The GR is expressed in almost every cell in the body and regulates genes controllingthe development, metabolism, and immune response. When the glucocorticoid receptor binds to glucocorticoids, its primar

3、ymechanism of action is the regulation of gene transcription. The unbound receptor resides in the cytosol of the cell. After thereceptor is bound to glucocorticoid, the receptor-glucorticoid complex can take either of two paths. The activated GR complexup-regulates the expression of anti-inflammator

4、y proteins in the nucleus or represses the expression of pro-inflammatory proteinsin the cytosol by preventing the translocation of other transcription factors from the cytosol into the nucleus. Dexamethasone is anagonist, and RU486 and cyproterone acetate are antagonists of the GR. Also, progestero

5、ne and DHEA have antagonist effects onthe GR.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Glucocorticoid Receptor.html Glucocorticoid HYPERLINK https:/www.MedChemE/Targets/Glucocorticoid Receptor.html HYPERLINK https:/www.MedChemE/Targets/Glucocorticoid Receptor.html Receptor HYPERLINK https

6、:/www.MedChemE/Targets/Glucocorticoid Receptor.html HYPERLINK https:/www.MedChemE/Targets/Glucocorticoid Receptor.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/Glucocorticoid Receptor.html HYPERLINK https:/www.MedChemE/Targets/Glucocorticoid Receptor.html Agonists, HYPERLINK https:/www.MedC

7、hemE/Targets/Glucocorticoid Receptor.html HYPERLINK https:/www.MedChemE/Targets/Glucocorticoid Receptor.html Antagonists, HYPERLINK https:/www.MedChemE/Targets/Glucocorticoid Receptor.html HYPERLINK https:/www.MedChemE/Targets/Glucocorticoid Receptor.html Activators HYPERLINK https:/www.MedChemE/Tar

8、gets/Glucocorticoid Receptor.html HYPERLINK https:/www.MedChemE/Targets/Glucocorticoid Receptor.html & HYPERLINK https:/www.MedChemE/Targets/Glucocorticoid Receptor.html HYPERLINK https:/www.MedChemE/Targets/Glucocorticoid Receptor.html Modulators HYPERLINK https:/www.MedChemE/_20S_-Protopanaxatriol

9、.html (20S)-Protopanaxatriol(20(S)-APPT; g-PPT) Cat. No.: HY-N0835 HYPERLINK https:/www.MedChemE/_S_-Mapracorat.html (S)-Mapracorat(S)-ZK-245186; (S)-BOL-303242X) Cat. No.: HY-14864A(20S)-Protopanaxatriol is a metabolite ofginsenoside. (20S)-Protopanaxatriol works throughthe glucocorticoid receptor

10、(GR) and oestrogenreceptor (ER), and is also a LXR inhibitor.(20S)-Protopanaxatriol shows a broad spectrum ofantitumor effects.(S)-Mapracorat is a selective and less activeglucocorticoid receptor agonist.Purity: 98.35%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg

11、Purity: 99.40%Clinical Data: No Development ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/21-acetoxypregna-1-4-9-11-16-tetraene-3-20-dione.html 21-Acetoxypregna-1,4,9(11),16-tetraene-3,20-dione HYPERLINK https:/www.MedChemE/21-acetoxypregna-1-4-9-11-16-tetraene-3-20-dione.html HYPERLINK ht

12、tps:/www.MedChemE/21-desacetyldeflazacort-d5.html 21-Desacetyldeflazacort-D5Cat. No.: HY-136340 Cat. No.: HY-100085S21-Acetoxypregna-1,4,9(11),16-tetraene-3,20-dioneis an intermediate of delta 9,11 steroidssynthesis, for example,Vamorolone (HY-109017). The delta 9,11steroids are modifications of glu

13、cocorticoids andhas anti-inflammatory properties.Purity: 99.84%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 25 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/AL-082D06.html AL HYPERLINK https:/www.MedChemE/AL-082D06.html HYP

14、ERLINK https:/www.MedChemE/AL-082D06.html 082D06(D06; D-06) Cat. No.: HY-15709 HYPERLINK https:/www.MedChemE/alclometasone.html Alclometasone(7a-Chloro-16a-methyl prednisolone) Cat. No.: HY-A0150AL 082D06 is a selective, nonsteroidalglucocorticoid receptor (GR) antagonist with Kof 210 nM.iAlclometas

15、one (7a-Chloro-16a-methyl prednisolone)is a glucocorticoid and inhibits the release ofpro-inflammatory mediators from leukocytes.Purity: 99.10%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HY

16、PERLINK https:/www.MedChemE/Amcinonide.html Amcinonide HYPERLINK https:/www.MedChemE/Amcinonide.html HYPERLINK https:/www.MedChemE/amcinonide-d4.html Amcinonide-d4(CL-34699) Cat. No.: HY-B1197 (CL-34699-d4) Cat. No.: HY-B1197SAmcinonide inhibit NO release from activatedmicroglia with IC50 3.38 nM. A

17、mcinonide hasaffinity for the glucocorticoid receptor.Amcinonide-d4 (CL-34699-d4) is the deuteriumlabeled Amcinonide. Amcinonide inhibit NO releasefrom activated microglia with IC 3.38 nM.50Amcinonide has affinity for the glucocorticoidreceptor.Purity: 99.61%Clinical Data: LaunchedSize: 10 mM 1 mL,

18、100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Amebucort.html Amebucort HYPERLINK https:/www.MedChemE/Amebucort.html HYPERLINK https:/www.MedChemE/AZD2906.html AZD2906Cat. No.: HY-U00298 Cat. No.: HY-113854Amebucort is a synthetic glucocorticoid

19、corticosteroid, may used for the research ofinflammatory disorders.AZD2906 is a selective glucocorticoid receptor(GR) agonist, increases micronucleated immatureerythrocytes in the bone marrow of rats. AZD2906shows IC s of 2.2, 0.3, 41.6 and 7.5 nM at GR in50human, rat PBMC and human, rat whole blood

20、,respectively.Purity: 98.04%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 20 mgPurity: 99.82%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/azd5423.html

21、 AZD5423 HYPERLINK https:/www.MedChemE/azd5423.html HYPERLINK https:/www.MedChemE/AZD9567.html AZD9567Cat. No.: HY-108243 Cat. No.: HY-120012AZD5423 is an inhaled, potent, selective, andnon-steroidal glucocorticoid receptor (GR)modulator (SGRM). AZD5423 effectively reducesallergen-induced responses

22、in subjects with mildallergic asthma.AZD9567 (compound 15) is a potent, oral active,non-steroidal and selective glucocorticoid receptormodulator (SGRM), with an IC of 3.8 nM.50Exhibits excellent efficacy in the streptococcalcell wall (SCW) reactivation model of jointinflammation.Purity: 99.85%Clinic

23、al Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.71%Clinical Data: Phase 2Size: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/bay-1003803.html BAY HYPERLINK https:/www.MedChemE/bay-1003803.html HYPERLINK https:/www.MedChemE/bay-1003803.html 1003803Cat. No.: HY-14535

24、1 HYPERLINK https:/www.MedChemE/Beclometasone.html Beclometasone(Beclomethasone) Cat. No.: HY-B1540BAY 1003803 is a glucocorticoid receptor agonistfor the topical treatment of psoriasis or severeatopic dermatitis.Beclometasone (Beclomethasone) is a prototypeglucocorticoid receptor agonist.Purity: 98

25、%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 95.44%Clinical Data: LaunchedSize: 10 mM 1 mL, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Beclometasone-dipropionate.html Beclometasone HYPERLINK https:/www.MedChemE/Beclometasone-dipropionate.html HYPERLINK https:/www.MedChemE/B

26、eclometasone-dipropionate.html dipropionate HYPERLINK https:/www.MedChemE/Beclometasone-dipropionate.html HYPERLINK https:/www.MedChemE/beclometasone-dipropionate-d10.html Beclometasone HYPERLINK https:/www.MedChemE/beclometasone-dipropionate-d10.html HYPERLINK https:/www.MedChemE/beclometasone-dipr

27、opionate-d10.html dipropionate-d10Cat. No.: HY-13571A Cat. No.: HY-13571AS1Betamethasone dipropionate, the prodrug ofBetamethasone, is an orally active and potentglucocorticoid with anti-inflammatory andimmunosuppressive activity. Betamethasone appearsto be an effective inhibitor of LPS-inducedinfla

28、mmation and MMP release.Beclometasone dipropionate-d10 is the deuteriumlabeled Beclometasone dipropionate. Betamethasonedipropionate, the prodrug of Betamethasone, is anorally active and potent glucocorticoid withanti-inflammatory and immunosuppressive activity.Purity: 99.92%Clinical Data: LaunchedS

29、ize: 10 mM 1 mL, 250 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/beclometasone-dipropionate-d6.html Beclometasone HYPERLINK https:/www.MedChemE/beclometasone-dipropionate-d6.html HYPERLINK https:/www.MedChemE/beclometasone-dipropionate-d6.html di

30、propionate-d6 HYPERLINK https:/www.MedChemE/beclometasone-dipropionate-d6.html HYPERLINK https:/www.MedChemE/beclomethasone-17-propionate.html Beclomethasone HYPERLINK https:/www.MedChemE/beclomethasone-17-propionate.html HYPERLINK https:/www.MedChemE/beclomethasone-17-propionate.html 17-propionateC

31、at. No.: HY-13571AS(Beclomethasone-17-monopropionate; 17-BMP) Cat. No.: HY-136239Beclometasone dipropionate-d6 is deuterium labeledBeclometasone dipropionate. Betamethasonedipropionate, the prodrug of Betamethasone, is anorally active and potent glucocorticoid withanti-inflammatory and immunosuppres

32、sive activity.Beclomethasone 17-propionate(Beclomethasone-17-monopropionate), an activemetabolite of Beclomethasone dipropionate(HY-13571), is a glucocorticoid receptor (GR)agonist.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize:

33、 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/beclomethasone-d5.html Beclomethasone-d5 HYPERLINK https:/www.MedChemE/beclomethasone-d5.html HYPERLINK https:/www.MedChemE/betamethasone.html BetamethasoneCat. No.: HY-B1540S Cat. No.: HY-13570Beclomethasone-d5 is the deuterium la

34、beledBeclometasone. Beclometasone (Beclomethasone) is aprototype glucocorticoid receptor agonist.Betamethasone is a synthetic glucocorticoid withanti-inflammatory and immunosuppressiveactivities. Betamethasone accelerates fetal lungmaturation and induces gene expression andapoptosis.Purity: 98%Clini

35、cal Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.97%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg, 500 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/betamethasone-acibutate.html Betamethasone HYPERLINK https:/www.MedChemE/betamethasone-acibutate.html HYPERLINK https:/www.MedChemE/betam

36、ethasone-acibutate.html acibutateCat. No.: HY-121062 HYPERLINK https:/www.MedChemE/Betamethasone_dipropionate.html Betamethasone HYPERLINK https:/www.MedChemE/Betamethasone_dipropionate.html HYPERLINK https:/www.MedChemE/Betamethasone_dipropionate.html dipropionate(Betamethasone 17,21-dipropionate)

37、Cat. No.: HY-13571Betamethasone acibutate, derives fromBetamethasone, is an acetate ester. Betamethasoneacibutate is a glucocorticoid.Betamethasone dipropionate is a glucocorticoidsteroid with anti-inflammatory andimmunosuppressive abilities.Purity: 98%Clinical Data: No Development ReportedSize: 1 m

38、g, 5 mgPurity: 98.31%Clinical Data: LaunchedSize: 10 mM 1 mL, 250 mg, 1 g HYPERLINK https:/www.MedChemE/betamethasone-dipropionate-d10.html Betamethasone HYPERLINK https:/www.MedChemE/betamethasone-dipropionate-d10.html HYPERLINK https:/www.MedChemE/betamethasone-dipropionate-d10.html dipropionate-d

39、10(Betamethasone 17,21-dipropionate-d10) Cat. No.: HY-13571S HYPERLINK https:/www.MedChemE/Betamethasone-hydrochloride.html Betamethasone HYPERLINK https:/www.MedChemE/Betamethasone-hydrochloride.html HYPERLINK https:/www.MedChemE/Betamethasone-hydrochloride.html hydrochlorideCat. No.: HY-13570ABeta

40、methasone dipropionate-d10 (Betamethasone17-d10,21-dipropionate-d10) is the deuteriumlabeled Betamethasone dipropionate. Betamethasonedipropionate is a glucocorticoid steroid withanti-inflammatory and immunosuppressive abilities.Betamethasone hydrochloride is a syntheticglucocorticoid with anti-infl

41、ammatory andimmunosuppressive activities. Betamethasonehydrochloride accelerates fetal lung maturationand induces gene expression and apoptosis.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/betamethas

42、one-valerate.html Betamethasone HYPERLINK https:/www.MedChemE/betamethasone-valerate.html HYPERLINK https:/www.MedChemE/betamethasone-valerate.html valerate(Betamethasone 17-valerate) Cat. No.: HY-B0727 HYPERLINK https:/www.MedChemE/betamethasone-d5.html Betamethasone-d5Cat. No.: HY-13570SBetamethas

43、one valerate (Betamethasone17-valerate), the 17-valerate ester ofBetamethasone, is a topical corticosteroid withanti-inflammatory activity. Betamethasone valerateis used in the treatment of recurrent aphthousstomatitis.Betamethasone-d5 is the deuterium labeledBetamethasone. Betamethasone is a synthe

44、ticglucocorticoid with anti-inflammatory andimmunosuppressive activities. Betamethasoneaccelerates fetal lung maturation and induces geneexpression and apoptosis.Purity: 99.14%Clinical Data: LaunchedSize: 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK

45、 https:/www.MedChemE/betamethasone-d5-1.html Betamethasone-d5-1 HYPERLINK https:/www.MedChemE/betamethasone-d5-1.html HYPERLINK https:/www.MedChemE/bi-653048.html BI HYPERLINK https:/www.MedChemE/bi-653048.html HYPERLINK https:/www.MedChemE/bi-653048.html 653048Cat. No.: HY-13570S1 Cat. No.: HY-1294

46、6Betamethasone-d5-1 is deuterium labeledBetamethasone. Betamethasone is a syntheticglucocorticoid with anti-inflammatory andimmunosuppressive activities. Betamethasoneaccelerates fetal lung maturation and induces geneexpression and apoptosis.Purity: 98%Clinical Data:Size: 1 mg, 5 mgBI 653048 is a se

47、lective and orally activenonsteroidal glucocorticoid (GC) agonistwith an IC value of 55 nM. BI 653048 inhibits50CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4isoforms activity and reduces affinity for thehERG ion channel (IC 30 M).50Purity: 98%Clinical Data: Phase 1Size: 1 mg, 5 mg HYPERLINK https:/www.M

48、edChemE/bi-653048-phosphate.html BI HYPERLINK https:/www.MedChemE/bi-653048-phosphate.html HYPERLINK https:/www.MedChemE/bi-653048-phosphate.html 653048 HYPERLINK https:/www.MedChemE/bi-653048-phosphate.html HYPERLINK https:/www.MedChemE/bi-653048-phosphate.html phosphate HYPERLINK https:/www.MedChe

49、mE/bi-653048-phosphate.html HYPERLINK https:/www.MedChemE/budesonide.html BudesonideCat. No.: HY-12946A Cat. No.: HY-13580BI 653048 phosphate is a selective and orallyactive nonsteroidal glucocorticoid(GC) agonist with an IC value of 55 nM.50Budesonide, an inhaled glucocortical steroid, isan orally

50、active glucocorticoid receptor agonist.Budesonide decreases the size of lung tumors,reverses DNA hypomethylation and modulates mRNAexpression of genes. Budesonide is ananti-inflammatory agent used for asthma.Purity: 98%Clinical Data: Phase 1Size: 1 mg, 5 mgPurity: 99.94%Clinical Data: LaunchedSize:

51、10 mM 1 mL, 100 mg, 200 mg, 500 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/budesonide-impurity-c.html Budesonide HYPERLINK https:/www.MedChemE/budesonide-impurity-c.html HYPERLINK https:/www.MedChemE/budesonide-impurity-c.html impurity HYPERLINK https:

52、/www.MedChemE/budesonide-impurity-c.html HYPERLINK https:/www.MedChemE/budesonide-impurity-c.html C HYPERLINK https:/www.MedChemE/budesonide-impurity-c.html HYPERLINK https:/www.MedChemE/budesonide-d8.html Budesonide-d8Cat. No.: HY-100087 Cat. No.: HY-13580SBudesonide impurity C is an impurity ofBud

53、esonide. Budesonide, an inhaled glucocorticalsteroid, is an orally active glucocorticoidreceptor agonist.Budesonide-d8 is the deuterium labeled Budesonide.Budesonide, an inhaled glucocortical steroid, isan orally active glucocorticoid receptor agonist.Budesonide decreases the size of lung tumors,rev

54、erses DNA hypomethylation and modulates mRNAexpression of genes.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/c108297.html C108297Cat. No.: HY-125096 HYPERLINK https:/www.MedChem

55、E/Ciclesonide.html Ciclesonide(RPR251526) Cat. No.: HY-B0625C108297 is a selective glucocorticoid receptor(GR) modulator (GR binding K 0.7 nM; GR reporterigene functional K 0.6 nM). C108297 attenuatesiobesity by reducing caloric intake and increasinglipolysis and fat oxidation, and in additionattenu

56、ates inflammation.Ciclesonide (RPR251526) is a glucocorticoid withan potent anti-inflammatory activity. Ciclesonidecan be used for asthma research.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.45%Clinical Data: LaunchedSize: 10 mM 1 mL, 50 mg, 100 mg HYPERLINK https:/ww

57、w.MedChemE/ciclesonide-d7.html Ciclesonide-d7 HYPERLINK https:/www.MedChemE/ciclesonide-d7.html HYPERLINK https:/www.MedChemE/clobetasone-butyrate.html Clobetasone HYPERLINK https:/www.MedChemE/clobetasone-butyrate.html HYPERLINK https:/www.MedChemE/clobetasone-butyrate.html butyrateCat. No.: HY-B06

58、25S Cat. No.: HY-B1616Ciclesonide-d7 is the deuterium labeledCiclesonide. Ciclesonide (RPR251526) is aglucocorticoid with an potent anti-inflammatoryactivity. Ciclesonide can be used for asthmaresearch.Clobetasone butyrate is a synthetic glucocorticoidand has topical anti-inflammatory activityespeci

59、ally in skin. Clobetasone butyrate can beused to relieve corticosteroid-responsivedermatoses, including atopic dermatitis andpsoriasis.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 10 mgPurity: 99.24%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg HYPERLINK https:/www.MedChemE/clobeta

60、sone-butyrate-d7.html Clobetasone HYPERLINK https:/www.MedChemE/clobetasone-butyrate-d7.html HYPERLINK https:/www.MedChemE/clobetasone-butyrate-d7.html butyrate-d7 HYPERLINK https:/www.MedChemE/clobetasone-butyrate-d7.html HYPERLINK https:/www.MedChemE/Corticosterone.html Corticosterone HYPERLINK ht