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MedKoo Cat#: 562794 | Name: NBI-35965 Mesylate
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

NBI-35965 Mesylate is a potent and selective corticotropin-releasing factor receptor 1 (CRF1) antagonist.

Chemical Structure

NBI-35965 Mesylate
NBI-35965 Mesylate
CAS#603151-83-3

Theoretical Analysis

MedKoo Cat#: 562794

Name: NBI-35965 Mesylate

CAS#: 603151-83-3

Chemical Formula: C22H26Cl2N4O3S

Exact Mass: 496.1103

Molecular Weight: 497.44

Elemental Analysis: C, 53.12; H, 5.27; Cl, 14.25; N, 11.26; O, 9.65; S, 6.45

Price and Availability

Size Price Availability Quantity
5mg USD 280.00
10mg USD 420.00
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Synonym
NBI-35965 Mesylate; NBI 35965 Mesylate; NBI35965 Mesylate;
IUPAC/Chemical Name
(7S)-6-(Cyclopropylmethyl)-2-(2,4-dichlorophenyl)-7-ethyl-7,8-dihydro-4-methyl-6H-1,3,6,8a-tetraazaacenaphthylene mesylate
InChi Key
ARENHXRYYRAMQA-RSAXXLAASA-N
InChi Code
InChI=1S/C21H22Cl2N4.CH4O3S/c1-3-15-11-27-21-18(26(15)10-13-4-5-13)8-12(2)24-20(21)19(25-27)16-7-6-14(22)9-17(16)23;1-5(2,3)4/h6-9,13,15H,3-5,10-11H2,1-2H3;1H3,(H,2,3,4)/t15-;/m0./s1
SMILES Code
CC1=CC2=C3N(N=C(C4=CC=C(Cl)C=C4Cl)C3=N1)C[C@H](CC)N2CC5CC5.OS(=O)(C)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
NBI-35965 Mesylate is a potent and selective corticotropin-releasing factor receptor 1 (CRF1) antagonist.
In vitro activity:
As a result of studies aimed at establishing a relationship between structure and CRF(1) binding affinity, NBI 35965 (12a) was identified as a high-affinity antagonist with a pK(i) value of 8.5. Compound 12a proved to be a functional CRF(1) antagonist with pIC(50) values of 7.1 and 6.9 in the in vitro CRF-stimulated cAMP accumulation and ACTH production assays, respectively, and 12a also reduced CRF or stress induced ACTH production in vivo. Reference: J Med Chem. 2005 Sep 8;48(18):5780-93. https://pubmed.ncbi.nlm.nih.gov/16134945/
In vivo activity:
This study examined the influence of repeated phasic CRDs and intracisternal (ic) CRF on the spontaneous discharge rate of LC neurons in chloral hydrate-anesthetized rats and the role of CRF receptors using the nonselective CRF(1)/CRF(2) antagonist, astressin, and the water-soluble CRF(1) receptor antagonist, NBI-35965. NBI-35965 (10 mg/kg, iv) prevented the 2nd CRD- and ic CRF-induced LC neuronal activation, while at 5 mg significantly reduced the LC response to the 2nd CRD by 80%, but did not block that of ic CRF injected 30 min later. Reference: Brain Res. 2005 Sep 14;1056(1):85-96. https://pubmed.ncbi.nlm.nih.gov/16095571/
Solvent mg/mL mM
Solubility
DMF 25.0 50.26
DMSO 25.0 50.26
Ethanol 10.0 20.10
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 497.44 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Gross RS, Guo Z, Dyck B, Coon T, Huang CQ, Lowe RF, Marinkovic D, Moorjani M, Nelson J, Zamani-Kord S, Grigoriadis DE, Hoare SR, Crowe PD, Bu JH, Haddach M, McCarthy J, Saunders J, Sullivan R, Chen T, Williams JP. Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists. J Med Chem. 2005 Sep 8;48(18):5780-93. doi: 10.1021/jm049085v. PMID: 16134945. 2. Hoare SR, Sullivan SK, Ling N, Crowe PD, Grigoriadis DE. Mechanism of corticotropin-releasing factor type I receptor regulation by nonpeptide antagonists. Mol Pharmacol. 2003 Mar;63(3):751-65. doi: 10.1124/mol.63.3.751. Erratum in: Mol Pharmacol. 2005 Jul;68(1):260. PMID: 12606786. 3. Ma H, Cui Z, Guo X, Zhao Q, Zhang Y, Guan Y, Yang P, Zhu H, Wang S, Zhang X, Zhang Y, Pan HL, Ma H. Corticotropin-releasing factor potentiates glutamatergic input and excitability of presympathetic neurons in the hypothalamus in spontaneously hypertensive rats. Neuropharmacology. 2023 Mar 15;230:109506. doi: 10.1016/j.neuropharm.2023.109506. Epub ahead of print. PMID: 36924924. 4. Kosoyan HP, Grigoriadis DE, Taché Y. The CRF(1) receptor antagonist, NBI-35965, abolished the activation of locus coeruleus neurons induced by colorectal distension and intracisternal CRF in rats. Brain Res. 2005 Sep 14;1056(1):85-96. doi: 10.1016/j.brainres.2005.07.010. PMID: 16095571.
In vitro protocol:
1. Gross RS, Guo Z, Dyck B, Coon T, Huang CQ, Lowe RF, Marinkovic D, Moorjani M, Nelson J, Zamani-Kord S, Grigoriadis DE, Hoare SR, Crowe PD, Bu JH, Haddach M, McCarthy J, Saunders J, Sullivan R, Chen T, Williams JP. Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists. J Med Chem. 2005 Sep 8;48(18):5780-93. doi: 10.1021/jm049085v. PMID: 16134945. 2. Hoare SR, Sullivan SK, Ling N, Crowe PD, Grigoriadis DE. Mechanism of corticotropin-releasing factor type I receptor regulation by nonpeptide antagonists. Mol Pharmacol. 2003 Mar;63(3):751-65. doi: 10.1124/mol.63.3.751. Erratum in: Mol Pharmacol. 2005 Jul;68(1):260. PMID: 12606786.
In vivo protocol:
1. Ma H, Cui Z, Guo X, Zhao Q, Zhang Y, Guan Y, Yang P, Zhu H, Wang S, Zhang X, Zhang Y, Pan HL, Ma H. Corticotropin-releasing factor potentiates glutamatergic input and excitability of presympathetic neurons in the hypothalamus in spontaneously hypertensive rats. Neuropharmacology. 2023 Mar 15;230:109506. doi: 10.1016/j.neuropharm.2023.109506. Epub ahead of print. PMID: 36924924. 2. Kosoyan HP, Grigoriadis DE, Taché Y. The CRF(1) receptor antagonist, NBI-35965, abolished the activation of locus coeruleus neurons induced by colorectal distension and intracisternal CRF in rats. Brain Res. 2005 Sep 14;1056(1):85-96. doi: 10.1016/j.brainres.2005.07.010. PMID: 16095571.