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EMMX Biotechnology LLC
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888-539-0666 |
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Product Name:NBI 35965 hydrochloride
CAS:603151-83-3
Purity:98% HPLC Package:5mg;10mg;25mg;50mg;100mg;250mg;500mg;1g
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| Company Name: |
Pharmacodia (Beijing) Co.,Ltd
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+86-400-851-9921 |
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sales@pharmacodia.com |
| Products Intro: |
Product Name:NBI-35965 Mesylate
CAS:603151-83-3
Package:10Mg-100g
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NBI 35965 hydrochloride manufacturers
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| | NBI 35965 hydrochloride Basic information |
| | NBI 35965 hydrochloride Chemical Properties |
| Melting point | 167 °C | | storage temp. | Store at -20°C | | solubility | Soluble in DMSO > 10 mM | | form | Powder |
| | NBI 35965 hydrochloride Usage And Synthesis |
| Uses | Corticotropin-releasing hormone, also known as corticotropin-releasing factor (CRF) or corticoliberin, is a peptide hormone and neurotransmitter involved in the stress response. It is secreted from the hypothalamus and is the major regulator of pituitary corticotropin-release and consequent glucocorticoid secretion. NBI 35965 is a selective CRF receptor 1 (CRF1) antagonist with a Ki value of 4 nM. It does not inhibit CRF2 (Ki = >10,000 nM). NBI 35965 inhibits cAMP accumulation and adrenocorticotropic hormone (ACTH) production in vitro (pIC50s = 7.1 and 6.9, respectively) and reduces CRF- and stress-induced ACTH production in vivo. In animal models of stress, NBI 35965 administration produces anxiolytic effects.[Cayman Chemical] | | Uses | NBI 35965 Mesylate is a selective corticotropin-releasing factor (CRF1) receptor antagonist involved in stress response. | | Uses | NBI 35965 Hydrochloride is a potent and selective corticotropin-releasing factor 1 (CRF1) antagonist. | | in vivo | NBI 35965 methanesulfonate (20 mg/kg; oral gavage; once) reduces stress induced ACTH production in mice[1].
In rats, NBI 35965 methanesulfonate (Compound 12a; 10 mg/kg) has a volume of distribution 17.8 L/kg, a plasma clearance of 17 mL/min/kg, and a half-life of 12 h. The estimated oral bioavailability is 34% with a mean maximal plasma concentration at 1 h of 560 ng/mL. NBI 35965 methanesulfonate also penetrated the blood-brain barrier, resulting in a mean maximal brain concentration of 700 ng/g[1]. | Animal Model: | Male CD-1 mice (24-26 g) bearing restraint stress[1] | | Dosage: | 20 mg/kg (10 mL/kg 5% mannitol-d (w/v) in water) | | Administration: | Oral gavage; 60 min prior to the initiation of the stressor | | Result: | Reduced stress induced ACTH production in vivo. |
| | IC 50 | CRFR1: 4 nM (Ki); CRFR1: 8.5 (pKi) |
| | NBI 35965 hydrochloride Preparation Products And Raw materials |
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