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11β-hydroxysteroid dehydrogenase type 1

" in MedChemExpress (MCE) Product Catalog:

By Targets:	11β-HSD (21) Amyloid-β (1) HIV (1)
By Research Areas:	Infection (1) Inflammation/Immunology (1) Metabolic Disease (19) Neurological Disease (4)

Inhibitors & Agonists

Recombinant Proteins

Isotope-Labeled Compounds

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-18056

PF-915275	11β-HSD	Metabolic Disease
PF-915275 is a potent, selective and orally active *human 11β-hydroxysteroid* dehydrogenase type 1 (11βHSD1) inhibitor with a K_i of 2.3 nM and an EC₅₀ of 15 nM (in HEK293 cells). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC₅₀** of 20 and 100 nM, respectively .

HY-18055

BVT-14225 1 Publications Verification	11β-HSD	Metabolic Disease
BVT-14225 is a selective 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with an IC₅₀ of 52 nM.

HY-18053

AZD 4017	11β-HSD	Metabolic Disease
AZD 4017 is a potent, selective 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) inhibitor, with an IC₅₀ of 7 nM.

HY-18173

AZD8329	11β-HSD	Metabolic Disease
AZD8329 is a potent 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with an IC₅₀ of 9 nM for human 11β-HSD1, displays excellent selectivity versus 11β-HSD2, 17β-HSD1 and 17β-HSD3 .

HY-19325

SKI2852	11β-HSD	Metabolic Disease
SKI2852 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with IC₅₀s of 1.6 nM and 2.9 nM against mHSD1 and hHSD1, respectively .

HY-111262

ABT-384	11β-HSD	Neurological Disease Metabolic Disease
ABT-384 is a potent, selective 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. ABT-384 exhibits high affinity (K_i 0.1-2.7 nM) against rodent, monkey, and human 11β-HSD1. ABT-384 blocks regeneration of active cortisol. ABT-384 can be used for the research of Alzheimer’s disease (AD) .

HY-101930A

(Rac)-BMS-816336	11β-HSD	Metabolic Disease
(Rac)-BMS-816336 (Compound 6n) is a racemate of BMS-816336. (Rac)-BMS-816336 is a potent inhibitor of human and *mouse 11β-hydroxysteroid* dehydrogenase type 1 (11β-HSD1) enzyme with IC₅₀**s of 10 nM and 68 nM, respectively. (Rac)-BMS-816336 has good metabolic stability .

HY-120496

Clofutriben ASP3662	11β-HSD	Neurological Disease Metabolic Disease
Clofutriben (ASP3662) is a selective, orally active and brain-penetrant **11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with K_i** values of 5.3 nM (human), 2.6 nM (mouse), and 23 nM (rat). Clofutriben inhibits conversion of inactive glucocorticoids to active glucocorticoids, reducing intracellular glucocorticoid exposure. Clofutriben ameliorates neuropathic pain, and restores muscle pressure thresholds in rodent models, while lacking effects in inflammatory pain .

HY-101930

BMS-816336	11β-HSD	Metabolic Disease
BMS-816336 is a novel, potent and orally bioavailable inhibitor against *human 11β-hydroxysteroid* dehydrogenase type 1 (11β-HSD1) enzyme with an IC₅₀** of 3.0 nM .

HY-122028

HSD-016	11β-HSD	Metabolic Disease
HSD-016 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with IC₅₀ values of 11, 1 and 8 nM against human, mouse and rat 11β-HSD1, respectively. HSD-016 can be used for type 2 diabetes research .

HY-117428

INU-101	11β-HSD	Metabolic Disease
INU-101 is a potent, selective and orally active **11β-hydroxysteroid dehydrogenase (11β-HSD*) type 1* inhibitor. INU-101 has highly potent inhibitory activity in mouse, monkey and human 11β-HSD1, derived from liver microsomes. INU-101 can enhance insulin sensitivity and lower the fasting blood glucose level. INU-101 can be used for the research of metabolic disease, such as diabetes .

HY-120643A

BMS-823778	11β-HSD	Metabolic Disease
BMS-823778 was developed as an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 to inhibit type 2 diabetes .

HY-18057

BVT-3498 AMG-311	11β-HSD	Metabolic Disease
BVT-3498 (AMG-311) is an inhibitor for 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) .

HY-B1588S

Carbenoxolone-d4	Amyloid-β HIV 11β-HSD	Infection Neurological Disease Inflammation/Immunology
Carbenoxolone-d₄ is deuterium labeled Carbenoxolone. Carbenoxolone, a semi-synthetic derivative of glycyrrhetinic acid, has previously been used for the management of dyspepsia and peptic ulcer because of its anti-inflammatory properties . Carbenoxolone, a general hemichannel and gap junction inhibitor, has the therapeutic potential of carbenoxolone in the research of chronic liver disease . Carbenoxolone is a suitable candidate for the inhibition of Aβ42 aggregation and the therapeutic potential of Cbx against AD . Carbenoxolone is small molecule Pannexin1 (Panx1,is an ATP release channel) inhibitor, attenuate Panx1 channel activity through modulation of the first extracellular loop .Carbenoxolone is an 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor that converts inactive glucocorticoid into an active form. Carbenoxolone has antiviral activity against DENV infection targeting the virus itself .

HY-117609

UE2343	11β-HSD	Neurological Disease
UE2343 is an orally available, brain-penetrant 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. UE2343 is being investigated for the treatment of Alzheimer's disease .

HY-161449

JTT-654	11β-HSD	Metabolic Disease
JTT-654 is an orally active, potent and selective11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. The IC₅₀ of JTT-654 for 11β-HSD1 is 4.65, 0.97, and 0.74 nM in human, rat, and mouse recombinant enzymes, respectively. JTT-654 showed competitive inhibition against human recombinant enzyme. The IC₅₀ value for human 11β-HSD2 is > 30 μM (human 11β-HSD2 is responsible for the reverse reaction against human 11β-HSD1). JTT-654 ameliorates insulin resistance and non-obese type 2 diabetes by inhibiting adipose tissue and liver 11β-HSD1 .

HY-162026

11β-HSD1-IN-14	11β-HSD	Metabolic Disease
11β-HSD1-IN-14 (Compound 17) is a selective inhibitor for 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1), with IC₅₀ of 74 nM for human HSD1, and 603 nM for HSD1 expressed HEK293 cell .

HY-10555

AMG-221	11β-HSD	Metabolic Disease
AMG-221 is an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) with a K_i of 12.8 nM in vitro biochemical scintillation proximity assay (SPA) and an IC₅₀ of 10.1 nM in cell-based assays . AMG-221 can be used for the research of type 2 diabetes .

HY-101930B

(R)-BMS-816336	11β-HSD	Metabolic Disease
(R)-BMS-816336 (Compound 6n-1) is a potent and orally active inhibitor of human, mouse and *cynomolgus monkey 11β-hydroxysteroid* dehydrogenase type 1 (11β-HSD1) enzyme with IC₅₀**s of 14.5 nM, 50.3 nM and 16 nM, respectively .

HY-18056R

PF-915275 (Standard)	11β-HSD	Metabolic Disease
PF-915275 (Standard) is the analytical standard of PF-915275. This product is intended for research and analytical applications. PF-915275 is a potent, selective and orally active human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor with a Ki of 2.3 nM and an EC50 of 15 nM (in HEK293 cells). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC50 of 20 and 100 nM, respectively .

HY-125421

11β-HSD1-IN-26	11β-HSD	Metabolic Disease
11β-HSD1-IN-26 (Compound 9f) is a type 1 11β-hydroxysteroid dehydrogenase (11β-HSD-1) inhibitor, with an IC₅₀ of 1.6 nM against the human form and 241 nM against the murine form. 11β-HSD1-IN-26 exhibits inhibitory activity against CYP1C19, with an IC₅₀ of 2 μM. 11β-HSD1-IN-26 can be used for research on metabolic syndrome .

Cat. No.	Compare	Product Name	Species	Source	Image

HY-P72237

	HSD11B1 Protein, Human (His-SUMO) 11 beta HSD 1; 11 beta HSD1 ; 11 beta hydroxysteroid dehydrogenase 1; 11 DH ; 11-beta hydroxysteroid dehydrogenase; type 1; 11-beta-HSD1; 11-DH; 11DH ; Corticosteroid 11 beta dehydrogenase isozyme 1; Corticosteroid 11-beta-dehydrogenase isozyme 1; CORTRD2; DHI1_HUMAN; HDL; HSD 11; HSD11; HSD11B; HSD11B1; HSD11L; member 1	Human	E. coli
	The proteins encoded by ED genes are involved in a variety of physiological processes. HSD11B1 Protein, Human (His-SUMO) is the recombinant human-derived HSD11B1 protein, expressed by E. coli , with N-6*His, N-SUMO labeled tag.

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HY-B1588S

Carbenoxolone-d4
Carbenoxolone-d₄ is deuterium labeled Carbenoxolone. Carbenoxolone, a semi-synthetic derivative of glycyrrhetinic acid, has previously been used for the management of dyspepsia and peptic ulcer because of its anti-inflammatory properties . Carbenoxolone, a general hemichannel and gap junction inhibitor, has the therapeutic potential of carbenoxolone in the research of chronic liver disease . Carbenoxolone is a suitable candidate for the inhibition of Aβ42 aggregation and the therapeutic potential of Cbx against AD . Carbenoxolone is small molecule Pannexin1 (Panx1,is an ATP release channel) inhibitor, attenuate Panx1 channel activity through modulation of the first extracellular loop .Carbenoxolone is an 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor that converts inactive glucocorticoid into an active form. Carbenoxolone has antiviral activity against DENV infection targeting the virus itself .

Carbenoxolone-d4

Carbenoxolone-d₄ is deuterium labeled Carbenoxolone. Carbenoxolone, a semi-synthetic derivative of glycyrrhetinic acid, has previously been used for the management of dyspepsia and peptic ulcer because of its anti-inflammatory properties . Carbenoxolone, a general hemichannel and gap junction inhibitor, has the therapeutic potential of carbenoxolone in the research of chronic liver disease . Carbenoxolone is a suitable candidate for the inhibition of Aβ42 aggregation and the therapeutic potential of Cbx against AD . Carbenoxolone is small molecule Pannexin1 (Panx1,is an ATP release channel) inhibitor, attenuate Panx1 channel activity through modulation of the first extracellular loop .Carbenoxolone is an 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor that converts inactive glucocorticoid into an active form. Carbenoxolone has antiviral activity against DENV infection targeting the virus itself .

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