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NVS-CRF38

CAS# 1207258-55-6

NVS-CRF38

Catalog No. BCC8059----Order now to get a substantial discount!

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Chemical structure

NVS-CRF38

3D structure

Chemical Properties of NVS-CRF38

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.
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.
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.

Biological Activity of NVS-CRF38

DescriptionNVS-CRF38 is a novel corticotropin-releasing factor receptor 1 (CRF1) antagonist with low water solubility. IC50 value: Target: CRF1 antagonist

References:
[1]. Stringer RA, et al. Preclinical metabolism and pharmacokinetics of NVS-CRF38, a potent and orally bioavailable corticotropin-releasing factor receptor 1 antagonist. Xenobiotica. 2014 Apr 3. [2]. Stringer RA, et al. 1-Aminobenzotriazole modulates oral drug pharmacokinetics through cytochrome P450 inhibition and delay of gastric emptying in rats. Drug Metab Dispos. 2014 Jul;42(7):1117-24.

NVS-CRF38 Dilution Calculator

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NVS-CRF38 Molarity Calculator

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Preparing Stock Solutions of NVS-CRF38

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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Background on NVS-CRF38

NVS-CRF38 is a novel corticotropin-releasing factor receptor 1 (CRF1) antagonist with low water solubility.

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References on NVS-CRF38

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.

Description

NVS-CRF38 is a novel corticotropin-releasing factor receptor 1 (CRF1) antagonist with low water solubility.

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