NBI 27914 hydrochloride

Pricing Availability   Qty
Cat.No. 1591 - NBI 27914 hydrochloride | C18H20Cl4N4.HCl | CAS No. 1215766-76-9
Description: Selective non-peptide CRF1 antagonist
Chemical Name: 5-Chloro-N-(cyclopropylmethyl)-2-methyl-N-propyl-N'-(2,4,6-trichlorophenyl)-4,6-pyrimidinediamine hydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations (12)
Reviews
Literature

Biological Activity

Selective, non-peptide corticotropin-releasing factor1 (CRF1) receptor antagonist (Ki = 1.7 nM); has no activity at CRF2 receptors. Blocks behavioral seizures in vivo.

Compound Libraries

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Technical Data

M. Wt 470.66
Formula C18H20Cl4N4.HCl
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 1215766-76-9
PubChem ID 45073446
InChI Key CPMGENCTAWBLNW-UHFFFAOYSA-N
Smiles Cl.CCCN(CC1CC1)C1=C(Cl)C(NC2=C(Cl)C=C(Cl)C=C2Cl)=NC(C)=N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
ethanol 43.42 100
DMSO 43.42 100

Preparing Stock Solutions

The following data is based on the product molecular weight 470.66. Batch specific molecular weights may vary from batch to batch due to solvent 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 2.12 mL 10.62 mL 21.25 mL
5 mM 0.42 mL 2.12 mL 4.25 mL
10 mM 0.21 mL 1.06 mL 2.12 mL
50 mM 0.04 mL 0.21 mL 0.42 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

Baram et al (1997) The CRF1 receptor mediates the excitatory actions of corticotropin releasing factor (CRF) in the developing rat brain: in vivo evidence using a novel, selective, non-peptide CRF receptor antagonist. Brain Res. 770 89 PMID: 9372207

Chen et al (1996) Design and synthesis of a series of non-peptide high-affinity human corticotropin-releasing factor1 receptor antagonists. J.Med.Chem. 39 4358 PMID: 8893829

McCarthy et al (1999) Recent advances with the CRF1 receptor: design of small molecule inhibitors, receptor subtypes and clinical indications. Curr.Pharm.Des. 5 289 PMID: 10213797


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Keywords: NBI 27914 hydrochloride, NBI 27914 hydrochloride supplier, Selective, non-peptide, CRF1, antagonists, Corticotropin-Releasing, Factor1, Receptors, NBI27914, hydrochloride, 1591, Tocris Bioscience

12 Citations for NBI 27914 hydrochloride

Citations are publications that use Tocris products. Selected citations for NBI 27914 hydrochloride include:

Jia et al (2013) Role of nesfatin-1 in a rat model of visceral hypersensitivity. Cereb Cortex 19 3487 PMID: 23801843

Wang et al (2011) CRF receptor antagonist astressin-B reverses and prevents alopecia in CRF over-expressing mice. PLoS One 6 e16377 PMID: 21359208

Gutknecht et al (2008) Expression, binding, and signaling properties of CRF2(a) receptors endogenously expressed in human retinoblastoma Y79 cells: passage-dependent regulation of functional receptors. J Neurochem 104 926 PMID: 17976162

Navarro et al (2015) Orexin-corticotropin-releasing factor receptor heteromers in the ventral tegmental area as targets for cocaine. Stroke 35 6639 PMID: 25926444

Gallopin et al (2006) Cortical sources of CRF, NKB, and CCK and their effects on pyramidal cells in the neocortex. J Neurosci 16 1440 PMID: 16339088

Lowery-Gionta et al (2012) Corticotropin releasing factor signaling in the central amygdala is recruited during binge-like ethanol consumption in C57BL/6J mice. J Neurosci 32 3405 PMID: 22399763

Silberman and Winder (2013) Corticotropin releasing factor and catecholamines enhance glutamatergic neurotransmission in the lateral subdivision of the central amygdala. Neuropharmacology 70 316 PMID: 23470280

Liu et al (2010) Differential actions of urocortins on neurons of the myenteric division of the enteric nervous system in guinea pig distal colon. Br J Pharmacol 159 222 PMID: 20002096

Delawary et al (2010) NMDAR2B tyrosine phosphorylation regulates anxiety-like behavior and CRF expression in the amygdala. Mol Brain 3 37 PMID: 21118530

Nakamura and Sapru (2009) Cardiovascular responses to microinjections of urocortins into the NTS: role of inotropic glutamate receptors. Am J Physiol Heart Circ Physiol 296 H2022 PMID: 19395554

Rajbhandari et al (2015) Predator Stress-Induced CRF Release Causes Enduring Sensitization of Basolateral Amygdala Norepinephrine Systems that Promote PTSD-Like Startle Abnormalities. J Neurosci 35 14270 PMID: 26490866

Ji et al (2013) Non-pain-related CRF1 activation in the amygdala facilitates synaptic transmission and pain responses. Mol Pain 9 2 PMID: 23410057


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