NVS-CRF38CAS# 1207258-55-6 |
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 1207258-55-6 | SDF | Download SDF |
| PubChem ID | 44816934 | Appearance | Powder |
| Formula | C19H21N5O2 | M.Wt | 351.4 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble in DMSO | ||
| Chemical Name | 7-(3,5-dimethyl-1,2,4-triazol-1-yl)-3-(4-methoxy-2-methylphenyl)-2,6-dimethylpyrazolo[5,1-b][1,3]oxazole | ||
| SMILES | CC1=C(C=CC(=C1)OC)C2=C(OC3=C(C(=NN23)C)N4C(=NC(=N4)C)C)C | ||
| Standard InChIKey | MEICIUGVENCLKP-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C19H21N5O2/c1-10-9-15(25-6)7-8-16(10)18-12(3)26-19-17(11(2)21-24(18)19)23-14(5)20-13(4)22-23/h7-9H,1-6H3 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | NVS-CRF38 is a novel corticotropin-releasing factor receptor 1 (CRF1) antagonist with low water solubility.
IC50 value:
Target: CRF1 antagonist References: | |||||
NVS-CRF38 Dilution Calculator
NVS-CRF38 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.8458 mL | 14.2288 mL | 28.4576 mL | 56.9152 mL | 71.144 mL |
| 5 mM | 0.5692 mL | 2.8458 mL | 5.6915 mL | 11.383 mL | 14.2288 mL |
| 10 mM | 0.2846 mL | 1.4229 mL | 2.8458 mL | 5.6915 mL | 7.1144 mL |
| 50 mM | 0.0569 mL | 0.2846 mL | 0.5692 mL | 1.1383 mL | 1.4229 mL |
| 100 mM | 0.0285 mL | 0.1423 mL | 0.2846 mL | 0.5692 mL | 0.7114 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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NVS-CRF38 is a novel corticotropin-releasing factor receptor 1 (CRF1) antagonist with low water solubility.
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Preclinical metabolism and pharmacokinetics of NVS-CRF38, a potent and orally bioavailable corticotropin-releasing factor receptor 1 antagonist.[Pubmed:24697490]
Xenobiotica. 2014 Oct;44(10):902-12.
1. The pharmacokinetic properties and metabolism of NVS-CRF38 [7-(3,5-dimethyl-1H-1,2,4-triazol-1-yl)-3-(4-methoxy-2-methylphenyl)-2,6-dimethyl pyrazolo[5,1-b]oxazole], a novel corticotropin-releasing factor receptor 1 (CRF1) antagonist, were determined in vitro and in animals. 2. NVS-CRF38 undergoes near complete absorption in rats and dogs. In both species the compound has low hepatic extraction and is extensively distributed to tissues. 3. In rat and human hepatic microsomes and cryopreserved hepatocytes from rat, dog, monkey and human, NVS-CRF38 was metabolised to form O-desmethyl NVS-CRF38 (M7) and several oxygen adducts (M1, M3, M4, M5 and M6). In hepatocytes further metabolites were observed, specifically the carboxylic acid (M2) and conjugates (sulphate and glucuronide) of M7. 4. Formation of primary metabolites in hepatocytes was blocked by the cytochrome P450 enzyme (P450) suicide inhibitor 1-aminobenzotriazole, implicating P450 enzymes in the primary metabolism of this compound. 5. NVS-CRF38 is weakly bound to plasma proteins from rat (fub = 0.19), dog (fub = 0.25), monkey (fub = 0.20) and humans (fub = 0.23). Blood-to-plasma partition for NVS-CRF38 approaches unity in rat and human blood. 6. The hepatic clearance of NVS-CRF38 in humans is predicted to be low (extraction ratio approximately 0.2) based on scaling from drug depletion profiles in hepatic microsomes.
