NBI-27914 HCl
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MedKoo CAT#: 525736

CAS#: 1215766-76-9 (HCl)

Description: NBI-27914 is a Corticotropin-Releasing Factor Antagonist of the CRF1 and CRF2 receptors (Corticotropin-releasing factor).

Chemical Structure

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NBI-27914 HCl
CAS# 1215766-76-9 (HCl)
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 525736
Name: NBI-27914 HCl
CAS#: 1215766-76-9 (HCl)
Chemical Formula: C18H21Cl5N4
Exact Mass: 432.04
Molecular Weight: 470.644
Elemental Analysis: C, 45.94; H, 4.50; Cl, 37.66; N, 11.90

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10mg USD 270
50mg USD 760
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Related CAS #: 184241-44-9 (free base)   1215766-76-9 (HCl)   847449-04-1 (xHCl)    

Synonym: NBI-27914; NBI 27914; NBI27914

IUPAC/Chemical Name: 5-Chloro-N4-(cyclopropylmethyl)-2-methyl-N4-propyl-N6-(2,4,6-trichlorophenyl)-4,6-pyrimidinediamine hydrochloride

InChi Key: CPMGENCTAWBLNW-UHFFFAOYSA-N

InChi Code: InChI=1S/C18H20Cl4N4.ClH/c1-3-6-26(9-11-4-5-11)18-15(22)17(23-10(2)24-18)25-16-13(20)7-12(19)8-14(16)21;/h7-8,11H,3-6,9H2,1-2H3,(H,23,24,25);1H

SMILES Code: ClC1=C(NC2=C(Cl)C(N(CC3CC3)CCC)=NC(C)=N2)C(Cl)=CC(Cl)=C1.[H]Cl

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, not in water

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
Certificate of Analysis:
View CoA: current batch, Lot#S8C02B02
Safety Data Sheet (SDS):
View Safety Data Sheet (SDS)
Instruction:
View handling instruction
Biological target: NBI-27914 (hydrochloride) is a selective Corticotropin-Releasing Factor 1 (CRF1) receptor antagonist with a Ki value of 1.7 nM.
In vitro activity: TBD
In vivo activity: Specifically, bilateral intra-dlBNST injections of the CRF type 1 receptor antagonist NBI27914 increased intra-nucleus accumbens dopamine release and induced reward-related behaviors in rats with chronic pain. Reference: Neurosci Lett. 2020 May 29;728:134958. https://pubmed.ncbi.nlm.nih.gov/32278943/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
Ethanol 43.4 92.26

Preparing Stock Solutions

The following data is based on the product molecular weight 470.64 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. Hara R, Asaoka Y, Takahashi D, Nomura H, Amano T, Minami M. Disappearance of the inhibitory effect of neuropeptide Y within the dorsolateral bed nucleus of the stria terminalis in rats with chronic pain. Neurosci Lett. 2020 May 29;728:134958. doi: 10.1016/j.neulet.2020.134958. Epub 2020 Apr 9. PMID: 32278943. 2. Ji G, Neugebauer V. Contribution of Corticotropin-Releasing Factor Receptor 1 (CRF1) to Serotonin Receptor 5-HT2CR Function in Amygdala Neurons in a Neuropathic Pain Model. Int J Mol Sci. 2019 Sep 6;20(18):4380. doi: 10.3390/ijms20184380. PMID: 31489921; PMCID: PMC6770811.
In vitro protocol: TBD
In vivo protocol: 1. Hara R, Asaoka Y, Takahashi D, Nomura H, Amano T, Minami M. Disappearance of the inhibitory effect of neuropeptide Y within the dorsolateral bed nucleus of the stria terminalis in rats with chronic pain. Neurosci Lett. 2020 May 29;728:134958. doi: 10.1016/j.neulet.2020.134958. Epub 2020 Apr 9. PMID: 32278943. 2. Ji G, Neugebauer V. Contribution of Corticotropin-Releasing Factor Receptor 1 (CRF1) to Serotonin Receptor 5-HT2CR Function in Amygdala Neurons in a Neuropathic Pain Model. Int J Mol Sci. 2019 Sep 6;20(18):4380. doi: 10.3390/ijms20184380. PMID: 31489921; PMCID: PMC6770811.

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1: Iarushkina NI, Bagaeva TR, Filaretova LP. [Effect of corticotropin releasing factor(CRF) on somatic pain sensitivity in conscious rats: involvement of CRF1 and CRF2 receptors]. Ross Fiziol Zh Im I M Sechenova. 2014 Nov;100(11):1287-96. Russian. PubMed PMID: 25665407.
2: Jia FY, Li XL, Li TN, Wu J, Xie BY, Lin L. Role of nesfatin-1 in a rat model of visceral hypersensitivity. World J Gastroenterol. 2013 Jun 14;19(22):3487-93. doi: 10.3748/wjg.v19.i22.3487. PubMed PMID: 23801843; PubMed Central PMCID: PMC3683689.
3: Chitravanshi VC, Kawabe K, Sapru HN. Mechanisms of cardiovascular actions of urocortins in the hypothalamic arcuate nucleus of the rat. Am J Physiol Heart Circ Physiol. 2013 Jul 15;305(2):H182-91. doi: 10.1152/ajpheart.00138.2013. Epub 2013 May 17. PubMed PMID: 23686711; PubMed Central PMCID: PMC3726959.
4: Carr JA, Zhang B, Li W, Gao M, Garcia C, Lustgarten J, Wages M, Smith EE. An intrinsic CRF signaling system within the optic tectum. Gen Comp Endocrinol. 2013 Jul 1;188:204-11. doi: 10.1016/j.ygcen.2013.03.020. Epub 2013 Apr 9. PubMed PMID: 23583471.
5: Ide S, Hara T, Ohno A, Tamano R, Koseki K, Naka T, Maruyama C, Kaneda K, Yoshioka M, Minami M. Opposing roles of corticotropin-releasing factor and neuropeptide Y within the dorsolateral bed nucleus of the stria terminalis in the negative affective component of pain in rats. J Neurosci. 2013 Apr 3;33(14):5881-94. doi: 10.1523/JNEUROSCI.4278-12.2013. PubMed PMID: 23554470.
6: Silberman Y, Winder DG. Corticotropin releasing factor and catecholamines enhance glutamatergic neurotransmission in the lateral subdivision of the central amygdala. Neuropharmacology. 2013 Jul;70:316-23. doi: 10.1016/j.neuropharm.2013.02.014. Epub 2013 Mar 5. PubMed PMID: 23470280; PubMed Central PMCID: PMC3644365.
7: Giardino WJ, Ryabinin AE. CRF1 receptor signaling regulates food and fluid intake in the drinking-in-the-dark model of binge alcohol consumption. Alcohol Clin Exp Res. 2013 Jul;37(7):1161-70. doi: 10.1111/acer.12076. Epub 2013 Feb 7. PubMed PMID: 23398267; PubMed Central PMCID: PMC3657581.
8: Gounko NV, Swinny JD, Kalicharan D, Jafari S, Corteen N, Seifi M, Bakels R, van der Want JJ. Corticotropin-releasing factor and urocortin regulate spine and synapse formation: structural basis for stress-induced neuronal remodeling and pathology. Mol Psychiatry. 2013 Jan;18(1):86-92. doi: 10.1038/mp.2012.43. Epub 2012 May 1. PubMed PMID: 22547117.
9: Miguel TT, Gomes KS, Nunes-de-Souza RL. Contrasting effects of nitric oxide and corticotropin- releasing factor within the dorsal periaqueductal gray on defensive behavior and nociception in mice. Braz J Med Biol Res. 2012 Apr;45(4):299-307. Epub 2012 Mar 29. PubMed PMID: 22450373; PubMed Central PMCID: PMC3854172.
10: Lowery-Gionta EG, Navarro M, Li C, Pleil KE, Rinker JA, Cox BR, Sprow GM, Kash TL, Thiele TE. Corticotropin releasing factor signaling in the central amygdala is recruited during binge-like ethanol consumption in C57BL/6J mice. J Neurosci. 2012 Mar 7;32(10):3405-13. doi: 10.1523/JNEUROSCI.6256-11.2012. PubMed PMID: 22399763; PubMed Central PMCID: PMC3307528.
11: Miguel TT, Nunes-de-Souza RL. Anxiogenic and antinociceptive effects induced by corticotropin-releasing factor (CRF) injections into the periaqueductal gray are modulated by CRF1 receptor in mice. Horm Behav. 2011 Aug;60(3):292-300. doi: 10.1016/j.yhbeh.2011.06.004. Epub 2011 Jun 23. PubMed PMID: 21723867.
12: Kang YM, Zhang AQ, Zhao XF, Cardinale JP, Elks C, Cao XM, Zhang ZW, Francis J. Paraventricular nucleus corticotrophin releasing hormone contributes to sympathoexcitation via interaction with neurotransmitters in heart failure. Basic Res Cardiol. 2011 May;106(3):473-83. doi: 10.1007/s00395-011-0155-2. Epub 2011 Feb 2. PubMed PMID: 21287352; PubMed Central PMCID: PMC3118407.
13: Singh R, Rai U. Immunomodulatory role of urotensins in teleost Channa punctatus. Gen Comp Endocrinol. 2011 Feb 1;170(3):613-21. doi: 10.1016/j.ygcen.2010.11.021. Epub 2010 Dec 2. PubMed PMID: 21130092.
14: Chitravanshi VC, Sapru HN. Microinjections of urocortin1 into the nucleus ambiguus of the rat elicit bradycardia. Am J Physiol Heart Circ Physiol. 2011 Jan;300(1):H223-9. doi: 10.1152/ajpheart.00391.2010. Epub 2010 Oct 15. PubMed PMID: 20952663; PubMed Central PMCID: PMC3023261.
15: Guan X, Wang L, Chen CL, Guan Y, Li S. Roles of two subtypes of corticotrophin-releasing factor receptor in the corticostriatal long-term potentiation under cocaine withdrawal condition. J Neurochem. 2010 Nov;115(3):795-803. doi: 10.1111/j.1471-4159.2010.06981.x. Epub 2010 Sep 28. PubMed PMID: 20807310.
16: Peng YL, Han RW, Chang M, Zhang L, Zhang RS, Li W, Han YF, Wang R. Central Neuropeptide S inhibits food intake in mice through activation of Neuropeptide S receptor. Peptides. 2010 Dec;31(12):2259-63. doi: 10.1016/j.peptides.2010.08.015. Epub 2010 Aug 26. PubMed PMID: 20800637.
17: Bhattacharya S, Subramanian G, Hall S, Lin J, Laoui A, Vaidehi N. Allosteric antagonist binding sites in class B GPCRs: corticotropin receptor 1. J Comput Aided Mol Des. 2010 Aug;24(8):659-74. doi: 10.1007/s10822-010-9364-2. Epub 2010 May 29. PubMed PMID: 20512399.
18: Liu XD, Fan HK, Zhang GH, Wang SC, Zhang Z, Feng PF. [Effects of CRF receptor antagonist on rem sleep in neonatal rat]. Zhongguo Ying Yong Sheng Li Xue Za Zhi. 2010 Feb;26(1):86-9. Chinese. PubMed PMID: 20476575.
19: Hummel M, Cummons T, Lu P, Mark L, Harrison JE, Kennedy JD, Whiteside GT. Pain is a salient "stressor" that is mediated by corticotropin-releasing factor-1 receptors. Neuropharmacology. 2010 Sep;59(3):160-6. doi: 10.1016/j.neuropharm.2010.05.001. Epub 2010 May 12. PubMed PMID: 20470804.
20: Liu S, Ren W, Qu MH, Bishop GA, Wang GD, Wang XY, Xia Y, Wood JD. Differential actions of urocortins on neurons of the myenteric division of the enteric nervous system in guinea pig distal colon. Br J Pharmacol. 2010 Jan;159(1):222-36. doi: 10.1111/j.1476-5381.2009.00516.x. Epub 2009 Nov 27. PubMed PMID: 20002096; PubMed Central PMCID: PMC2823367.