NBI 35965 hydrochloride

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Cat.No. 3100 - NBI 35965 hydrochloride | C21H22Cl2N4.HCl | CAS No. 1782228-59-4
Description: Potent and selective CRF1 antagonist
Chemical Name: (7S)-6-(Cyclopropylmethyl)-2-(2,4-dichlorophenyl)-7-ethyl-7,8-dihydro-4-methyl-6H-1,3,6,8a-tetraazaacenaphthylene hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (2)
Reviews
Literature (3)

Biological Activity

Potent and selective corticotropin-releasing factor receptor 1 (CRF1) antagonist (Ki values are 4 and > 10000 nM at CRF1 and CRF2 respectively). Inhibits cAMP accumulation and adrenocorticotropic hormone (ACTH) production in vitro (pIC50 values are 7.1 and 6.9 respectively) and attenuates CRF and ACTH production in vivo. Orally active and brain penetrant with anxiolytic activity.

Compound Libraries

NBI 35965 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 437.79
Formula C21H22Cl2N4.HCl
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 1782228-59-4
PubChem ID 71433630
InChI Key LNYUWBPFYXPUIO-RSAXXLAASA-N
Smiles CC[C@@H]3N(CC5CC5)C1=C2C(C(C4=CC=C(Cl)C=C4Cl)=NN2C3)=NC(C)=C1.Cl

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

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 43.78 100
DMSO 43.78 100

Preparing Stock Solutions

The following data is based on the product molecular weight 437.79. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.28 mL 11.42 mL 22.84 mL
5 mM 0.46 mL 2.28 mL 4.57 mL
10 mM 0.23 mL 1.14 mL 2.28 mL
50 mM 0.05 mL 0.23 mL 0.46 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.

Million et al (2003) A novel water-soluble selective CRF1 receptor antagonist, NBI 35965, blunts stress-induced visceral hyperalgesia and colonic motor function in rats. Brain Res. 985 32 PMID: 12957366

Hoare et al (2003) Mechanism of corticotropin-releasing factor type I receptor regulation by non-peptide antagonists. Mol.Pharmacol. 63 751 PMID: 12606786

Gross et al (2005) Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists. J.Med.Chem. 48 5780 PMID: 16134945


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Keywords: NBI 35965 hydrochloride, NBI 35965 hydrochloride supplier, NBI35965, CRF1R, CRF, 1, receptor, antagonist, corticotropin-releasing, factor, antagonists, CRF1, Receptors, 3100, Tocris Bioscience

2 Citations for NBI 35965 hydrochloride

Citations are publications that use Tocris products. Selected citations for NBI 35965 hydrochloride include:

Martinon and Dabrowska (2018) Corticotropin-Releasing Factor Receptors Modulate OXT Release in the Dorsolateral Bed Nucleus of the Stria Terminalis (BNST) in Male Rats. Front Neurosci 12 183 PMID: 29618970

Abdelhamid et al (2013) Forced swim-induced musculoskeletal hyperalgesia is mediated by CRF2 receptors but not by TRPV1 receptors. Neuropharmacology 72 29 PMID: 23624287


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Literature in this Area

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