NBI 27914 Free Base | CAS# 184241-44-9 (free base) | Corticotropin-Releasing Factor Antagonist

NBI 27914 Free Base
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 414288

CAS#: 184241-44-9 (free base)

Description: NBI 27914 Free Base is a Corticotropin-Releasing Factor Antagonist

Chemical Structure

NBI 27914 Free Base

CAS# 184241-44-9 (free base)

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 414288
Name: NBI 27914 Free Base
CAS#: 184241-44-9 (free base)
Chemical Formula: C18H20Cl4N4
Exact Mass: 432.04
Molecular Weight: 434.186
Elemental Analysis: C, 49.79; H, 4.64; Cl, 32.66; N, 12.90

Price and Availability

Size	Price	Availability
10mg	USD 335	2 Weeks
50mg	USD 942	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Related CAS #: 184241-44-9 (free base) 1215766-76-9 (HCl) 847449-04-1 (xHCl)

Synonym: NBI 27914 Free Base; NBI27914; NBI-27914

IUPAC/Chemical Name: 4,6-Pyrimidinediamine, 5-chloro-N-(cyclopropylmethyl)-2-methyl-N-propyl-n-(2,4,6-trichlorophenyl)

InChi Key: GWLHYBQAZOGDLX-UHFFFAOYSA-N

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

SMILES Code: ClC1=C(N(CCC)C2=NC(C)=NC(NCC3CC3)=C2Cl)C(Cl)=CC(Cl)=C1

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: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

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-27914 is a potent and selective antagonist of CRFR1.
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/

Preparing Stock Solutions

The following data is based on the product molecular weight 434.19 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.

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: 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. PMID: 20512399.

2: Prater CM, Harris BN, Carr JA. Tectal CRFR1 receptor involvement in avoidance and approach behaviors in the South African clawed frog, Xenopus laevis. Horm Behav. 2020 Apr;120:104707. doi: 10.1016/j.yhbeh.2020.104707. Epub 2020 Feb 6. PMID: 32001211.

3: Martínez V, Taché Y. Role of CRF receptor 1 in central CRF-induced stimulation of colonic propulsion in rats. Brain Res. 2001 Mar 2;893(1-2):29-35. doi: 10.1016/s0006-8993(00)03277-7. PMID: 11222989.

4: Kubo Y, Kumano A, Kamei K, Amagase K, Abe N, Takeuchi K. Urocortin prevents indomethacin-induced small intestinal lesions in rats through activation of CRF2 receptors. Dig Dis Sci. 2010 Jun;55(6):1570-80. doi: 10.1007/s10620-009-0930-1. Epub 2009 Aug 26. PMID: 19707872.

5: Yarushkina NI, Filaretova LP. The peripheral corticotropin-releasing factor (CRF)-induced analgesic effect on somatic pain sensitivity in conscious rats: involving CRF, opioid and glucocorticoid receptors. Inflammopharmacology. 2018 Apr;26(2):305-318. doi: 10.1007/s10787-018-0445-5. Epub 2018 Feb 5. PMID: 29404882.

6: Zhu J, Chen Z, Tian J, Meng Z, Ju M, Wu G, Tian Z. miR-34b attenuates trauma- induced anxiety-like behavior by targeting CRHR1. Int J Mol Med. 2017 Jul;40(1):90-100. doi: 10.3892/ijmm.2017.2981. Epub 2017 May 9. PMID: 28498394; PMCID: PMC5466391.

7: Prater CM, Harris BN, Carr JA. Tectal CRFR1 receptors modulate food intake and feeding behavior in the South African clawed frog Xenopus laevis. Horm Behav. 2018 Sep;105:86-94. doi: 10.1016/j.yhbeh.2018.07.013. Epub 2018 Aug 8. PMID: 30077740.

8: 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. PMID: 20470804.

9: 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. PMID: 23801843; PMCID: PMC3683689.

10: 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.

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NBI 27914 Free Base featured