| Company Name: |
SPIRO PHARMA |
| Tel: |
|
| Email: |
eric_feng1954@126.com |
| Company Name: |
BOC Sciences |
| Tel: |
16314854226 |
| Email: |
info@bocsci.com |
(2R)-3-Cyclopentyl-2-[4-(methanesulfonyl)phenyl]-N-(thiazol-2-yl)propionamide manufacturers
- RO-28-1675
-
- $396.00
-
2026-05-11
- CAS:300353-13-3
- Purity: 98.13%
- Supply Ability: 10g
|
| | (2R)-3-Cyclopentyl-2-[4-(methanesulfonyl)phenyl]-N-(thiazol-2-yl)propionamide Basic information |
| | (2R)-3-Cyclopentyl-2-[4-(methanesulfonyl)phenyl]-N-(thiazol-2-yl)propionamide Chemical Properties |
| density | 1.306 | | storage temp. | Store at -20°C | | solubility | DMSO : 50 mg/mL (132.10 mM; Need ultrasonic) | | form | Powder | | pka | 8.65±0.50(Predicted) | | color | White to off-white | | InChI | 1S/C18H22N2O3S2/c1-25(22,23)15-8-6-14(7-9-15)16(12-13-4-2-3-5-13)17(21)20-18-19-10-11-24-18/h6-11,13,16H,2-5,12H2,1H3,(H,19,20,21)/t16-/m1/s1 | | InChIKey | NEQSWPCDHDQINX-MRXNPFEDSA-N | | SMILES | [S](=O)(=O)(C)c1ccc(cc1)[C@@H](CC3CCCC3)C(=O)Nc2[s]ccn2 |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids |
| | (2R)-3-Cyclopentyl-2-[4-(methanesulfonyl)phenyl]-N-(thiazol-2-yl)propionamide Usage And Synthesis |
| Uses | A cell-permeable thiazolyl-propanamide compound that acts as an allosteric glucokinase-(GK) selective activator, increasing Vmax and decreasing [S]1/2 (by 1.5- and 4.3-fold, respectively, at 3 µM; [Glucose] = 5 mM) in human GK enzymatic assays, as well as freeing GK from the inhibitory action of GK regulatory protein (GKRP), resulting in increased GK nuclear-to-cytosol translocation in primary rat hepatocytes (EC50/[Glucose] = 0.16 µM/16.8 mM, 0.27 µM/8.4 mM, 2.2 µM/2.8 mM) and reduced glucose concentration for stimulating insulin secretion from isolated rat pancreatic islets (threshold [glucose] = 3 mM vs 6 mM with or without 3 µM Ro-28-1675). Exhibits in vivo glucose-lowering and insulin-releasing activity in non-diabetic C57BL/6 mice and Wistar rats and is efficacious in several murine (KK/Upj-Ay/J, ob/ob, and diet-induced obese C57BL/6) and rodent (Goto-Kakizaki) type II diabetes mellitus (T2DM) models (10 to 50 mg/kg via p.o.), while efficacy is no longer observed in older hypoinsulinemic db/db mice with blood glucose levels reaching 300 mg/dl. Reported not to affect the activity of hexokinase I or II and display no activity toward GK-independent insulin release from β cells upon 2-Ketoisocaproic acid (α-KIC) stimulation. | | Definition | ChEBI: (2R)-3-cyclopentyl-2-(4-methylsulfonylphenyl)-N-(2-thiazolyl)propanamide is a member of acetamides. | | Biological Activity | RO-28-1675 is a potent allosteric activator of glucokinase with EC50 of 54 nM. It can be used in type 2 diabetes research. | | in vitro | RO-28-1675 can reverse the inhibitory action of the human glucokinase regulatory protein (GKRP).
| | in vivo | RO-28-1675 (50 mg/kg; po) reduces blood glucose levels in wild-type C57BL/6J mice.
RO-28-1675 (10 mg/kg; po) displays lower clearance and higher oral bioavailability.
| Animal Model: | 10 weeks old male C57BL/6J mice | | Dosage: | 50 mg/kg | | Administration: | Oral administration | | Result: | Reduced blood glucose levels. | | Animal Model: | C57BL/6J mice | | Dosage: | 10 mg/kg | | Administration: | Oral administr ation | | Result: | AUC 0-inf (5150 ng h/mL), C max (1140 μg/mL) , T max (3.3 hours ), F po (92.8%) with 10 mg/kg orally administered. | | | target | EC50: 54 nM (glucokinase) |
| | (2R)-3-Cyclopentyl-2-[4-(methanesulfonyl)phenyl]-N-(thiazol-2-yl)propionamide Preparation Products And Raw materials |
|