| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
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Purity: ≥98%
Ro 28-1675 (Ro-0281675) is a novel, potent and allosteric GK activator with a SC1.5 value of 0.24± 0.0019 uM. Ro 28-1675 reduced fasting and postprandial glucose levels following an OGTT, was well tolerated, and displayed no adverse effects related to drug administration other than hypoglycemia at the maximum dose (400 mg).
| ln Vitro |
The inhibitory impact of human glucokinase regulating protein (GKRP) can be counteracted by RO-28-1675 [2].
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|---|---|
| ln Vivo |
In wild-type C57BL/6J mice, RO-28-1675 (50 mg/kg; oral) lowers blood glucose levels [2]. Following oral treatment (10 mg/kg), RO-28-1675 has a high oral bioavailability (92.8% in mice) and Cmax (1140 μg/mL).
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| Animal Protocol |
Animal/Disease Models: 10weeks old male C57BL/6J mice [2]
Doses: 50 mg/kg Route of Administration: Oral Experimental Results:Lower blood sugar levels. Animal/Disease Models: C57BL/6J mice[1] Doses: 10 mg/kg (pharmacokinetic/PK/PK analysis Route of Administration: Oral Experimental Results:Oral bioavailability (92.8%), Cmax (1140 μg/mL), T max ( 3.3h). |
| References |
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| Additional Infomation |
(2R)-3-cyclopentyl-2-(4-methylsulfonylphenyl)-N-(2-thiazolyl)propanamide is a member of acetamides.
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| Molecular Formula |
C18H22N2O3S2
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|---|---|
| Molecular Weight |
378.50888
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| Exact Mass |
378.107
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| CAS # |
300353-13-3
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| PubChem CID |
9886086
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| Appearance |
White to off-white solid powder
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| LogP |
5.003
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
25
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| Complexity |
547
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CS(=O)(=O)C1=CC=C(C=C1)[C@@H](CC2CCCC2)C(=O)NC3=NC=CS3
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| InChi Key |
NEQSWPCDHDQINX-MRXNPFEDSA-N
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| InChi Code |
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
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| Chemical Name |
(2R)-3-Cyclopentyl-2-[4-(methanesulfonyl)phenyl]-N-(thiazol-2-yl)propionamide
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| Synonyms |
RO28-1675 RO-28-1675 RO 28-1675 RO028-1675 RO-028-1675 RO 028-1675
RO281675 RO 281675 RO-281675 Ro 0281675 Ro-0281675 Ro0281675.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~132.10 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.60 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.60 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.60 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6419 mL | 13.2097 mL | 26.4194 mL | |
| 5 mM | 0.5284 mL | 2.6419 mL | 5.2839 mL | |
| 10 mM | 0.2642 mL | 1.3210 mL | 2.6419 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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