SKI-2852
- CAS No.
- 1346554-47-9
- Chemical Name:
- SKI-2852
- Synonyms
- SKI-2852;4-Pyrimidinecarboxamide, 2-[(2R)-4-[2-fluoro-4-(methylsulfonyl)phenyl]-2-methyl-1-piperazinyl]-N-[5-hydroxytricyclo[3.3.1.13,7]dec-2-yl]-
- CBNumber:
- CB55867322
- Molecular Formula:
- C27H34FN5O4S
- Molecular Weight:
- 543.65
- MDL Number:
- MOL File:
- 1346554-47-9.mol
- MSDS File:
- SDS
- TDS File:
- TDS
SKI-2852 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 45303 | SKI2852 ≥98% | 1346554-47-9 | 1mg | $55 | 2026-04-30 | Buy |
| Cayman Chemical | 45303 | SKI2852 ≥98% | 1346554-47-9 | 5mg | $151 | 2026-04-30 | Buy |
| Cayman Chemical | 45303 | SKI2852 ≥98% | 1346554-47-9 | 10mg | $248 | 2026-04-30 | Buy |
| ChemScene | CS-0015132 | SKI2852 98.41% | 1346554-47-9 | 5mg | $173 | 2026-06-04 | Buy |
| ChemScene | CS-0015132 | SKI2852 98.41% | 1346554-47-9 | 10mg | $277 | 2026-06-04 | Buy |
SKI-2852 Chemical Properties,Uses,Production
Description
SKI2852 is a Highly Potent, Selective, and Orally Bioavailable Inhibitor of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) potentially for treatment of diabetics. SKI2852 bioactivity data: hHSD1 IC50 = 2.9nM; mHSD1 IC50 = 1.6nM; HEK293 IC50 = 4/4 nM; Mous PK: F = 96%; CYP3A4 IC50 > 10 μM; CYP2C19 IC50 > 10 μM. SKI2852 demonstrated no CYP and PXR liabilities, excellent PK profiles across species, and highly potent and sustainable PD activity. Repeated oral administration of SKI2852 significantly reduced blood glucose and HbA1c levels and improved the lipid profiles in ob/ob mice.
Uses
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[1].
in vivo
SKI2852 (20 mg/kg; oral; once daily for 25 days) significantly reduces blood glucose and HbA1c levels and improved the lipid profiles in ob/ob mice[1].
In Vivo PK Data for SKI2852[1]
| species | iva | pob | ||||||
| CL (L/kg/h) | Vss (L/kg) | t1/2 (h) | AUC (μg × h/mL) | Cmax (μg/mL) | tmax (h) | AUC (μg × h/mL) | F (%) | |
| mousec | 0.42 | 1.1 | 1.7 | 2.35 | 2.21 | 1.0 | 11.26 | 96 |
| ratc | 0.93 | 2.1 | 1.8 | 1.12 | 1.02 | 1.3 | 3.39 | 60 |
| dogd | 0.36 | 2.4 | 4.7 | 1.47 | 1.12 | 2.1 | 11.52 | 98 |
a10% hydroxylpropyl-β-cyclodextrin was used as vehicle. b0.5% methylcellulose and 1% Tween80 was used as vehicle. cDosed iv at 1 mg/kg, po at 5mg/kg. dDosed iv at 0.5 mg/kg, po at 4 mg/kg.
| Animal Model: | ob/ob mice, diet-induced obesity (DIO) model[1] |
| Dosage: | 20 mg/kg |
| Administration: | Oral, once daily for 25 days |
| Result: | Efficiently reduced postprandial glucose and/or blood HbA1c levels and suppressed hepatic mRNA levels of gluconeogenic enzymes. Clearly enhanced hepatic and whole-body insulin sensitivities in a hyperinsulinemic-euglycemic clamp experiment in DIO mice. |
| Animal Model: | C57BL/6 mice, rats and dogs[1] |
| Dosage: | 0.5 or 4 mg/kg |
| Administration: | IV or PO (Pharmacokinetic Analysis) |
| Result: | Showed good pharmacokinetic profiles. |
References
[1] Ryu JH, et al. Discovery of 2-((R)-4-(2-Fluoro-4-(methylsulfonyl)phenyl)-2-methylpiperazin-1-yl)-N-((1R,2s,3S,5S,7S)-5-hydroxyadamantan-2-yl)pyrimidine-4-carboxamide (SKI2852): A Highly Potent, Selective, and Orally Bioavailable Inhibitor of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1). J Med Chem. 2016 Nov 23;59(22):10176-10189. DOI:10.1021/acs.jmedchem.6b01122
SKI-2852 Preparation Products And Raw materials
Raw materials
Preparation Products
SKI-2852 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Shanghai Chaolan Chemical Technology Center | QQ：65489617 13301690235 | Sales@ATKchemical.com | China | 9699 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +1-00000000000 | marketing@targetmol.com | United States | 32431 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6288 | 58 |
| Suzhou Chenrui Biotechnology Co. LTD | 17625585511 | 1580084073@qq.com | China | 990 | 58 |
| Beijing Jin Ming Biotechnology Co., Ltd. | 010-60605840 | psaitong@jm-bio.com | China | 27626 | 58 |
| Hubei Kele Fine Chemical Co., Ltd | 027-59101668 19945030958 | 2223443625@qq.com | China | 7996 | 58 |
| TargetMol Chemicals Inc. | 4008200310 15002144251 | marketing@tsbiochem.com | China | 24951 | 58 |
| https://hanhongsci.com/ | 021-54306202 18917919676 | info@hanhongsci.com | China | 29982 | 58 |
| Jiangsu Aikon Biopharmaceutical R&D Co.,Ltd. | 025-66061636 19370895928 | qqyang@aikonchem.com | China | 9995 | 58 |
| Shanghai Amole Biotechnology Co., Ltd. | 13370042665 18916960931 | 2596183085@qq.com | China | 17234 | 58 |
