SKI2852 free base · Synonyms: SKI-2852 · SKI 2852
SKI2852 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase type 1 inhibitor.
For research use only. Not for human or veterinary use.
SKI2852 structure
CAS No.: 1346554-47-9
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 25 mg | USD 420.00 | BP-02187-25mg | In stock | Get quote |
| 50 mg | USD 670.00 | BP-02187-50mg | In stock | Get quote |
| 100 mg | USD 1,060.00 | BP-02187-100mg | In stock | Get quote |
| 250 mg | USD 2,150.00 | BP-02187-250mg | In stock | Get quote |
| 500 mg | USD 3,400.00 | BP-02187-500mg | In stock | Get quote |
Need another size or custom synthesis? Request a quote.
Description
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 .
Biological activity
In Vitro SKI2852 inhibits 11β-HSD1 with an IC50 of 4.4 ± 0.5 nM in HEK293 cells stably transfected with human 11β-HSD1 cDNA. The amide carbonyl group of SKI2852 established a central hydrogen bond interaction with the hydroxyl side chain of Ser170, one of the key residues (Ser170, Tyr183, and Lys 187) that define the catalytic triad for 11β-HSD1 activity. 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.
Identifiers
- SMILES
-
O=C(C1=NC(N2[C@H](C)CN(C3=CC=C(S(=O)(C)=O)C=C3F)CC2)=NC=C1)N[C@@H]4[C@]5([H])C[C@@]6([H])C[C@](C5)(O)C[C@]4([H])C6 - InChIKey
-
SSKKTEYBWOVEET-MYCXXBLFSA-N
Specifications
- MW (average)
- 543.6530
- Formula
- C27H34FN5O4S
- CAS No.
- 1346554-47-9
- Physical state
- Solid
- Color
- White to off-white
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder -20℃ 3 years; 4℃ 2 years; In solvent -20℃ 1 month;
Solubility
soluble in DMSO