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Submit ReviewCP 99994 dihydrochloride
Description: High affinity NK1 antagonist
Chemical Name: (2S,3S)-N-[(2-Methoxyphenyl)methyl]-2-phenyl-3-piperidinamine dihydrochloride
Purity: ≥99% (HPLC)
Biological Activity for CP 99994 dihydrochloride
CP 99994 dihydrochloride is a high affinity NK1 antagonist (Ki = 0.145 nM in vitro). Also displays high ex vivo binding potency in gerbil striatum (IC50 = 36.8 nM). Attenuates endothelium-dependent contraction induced by substance P.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Compound Libraries for CP 99994 dihydrochloride
CP 99994 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for CP 99994 dihydrochloride
| M. Wt | 369.33 |
| Formula | C19H24N2O.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 145148-39-6 |
| PubChem ID | 68466923 |
| InChI Key | WNHRFWPLRATIDT-FFUVTKDNSA-N |
| Smiles | COC(C=CC=C3)=C3CN[C@@H]1[C@H]([C@]2=CC=CC=C2)NCCC1.Cl.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 for CP 99994 dihydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 36.93 | 100 | |
| DMSO | 18.47 | 50 |
Preparing Stock Solutions for CP 99994 dihydrochloride
The following data is based on the product molecular weight 369.33. 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 | 2.71 mL | 13.54 mL | 27.08 mL |
| 5 mM | 0.54 mL | 2.71 mL | 5.42 mL |
| 10 mM | 0.27 mL | 1.35 mL | 2.71 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
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Product Datasheets for CP 99994 dihydrochloride
References for CP 99994 dihydrochloride
References are publications that support the biological activity of the product.
Shirahase et al (1995) Endothelium-dependent contraction in intrapulmonary arteries: mediation by endothelial NK1 receptors and TXA2. Br.J.Pharmacol. 115 1215 PMID: 7582548
Duffy et al (2002) Correlation of neurokinin (NK) 1 receptor occupancy in gerbil striatum with behavioral effects of NK1 antagonists. J.Pharmacol.Exp.Ther. 301 536 PMID: 11961054
Lindstrom et al (2007) Neurokinin 1 receptor antagonists: correlation between in vitro receptor interaction and in vivo efficacy. J.Pharmacol.Exp.Ther. 322 1286 PMID: 17575073
If you know of a relevant reference for CP 99994 dihydrochloride, please let us know.
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Keywords: CP 99994 dihydrochloride, CP 99994 dihydrochloride supplier, pfizer, CP99994, neurokinin, 1, receptors, nk1, tachykinin, substance, p, antagonists, NK1, Receptor, 3417, Tocris Bioscience
7 Citations for CP 99994 dihydrochloride
Citations are publications that use Tocris products. Selected citations for CP 99994 dihydrochloride include:
Horn et al (2013) Novel dynamic measures of emetic behavior in musk shrews. Nature 179 60 PMID: 23953843
Wei et al (2015) Differential Gene Expression Profile in the Rat Caudal Vestibular Nucleus is Associated with Individual Differences in Motion Sickness Susceptibility. PLoS One 10 e0124203 PMID: 25910039
Craig L et al (2021) Role of perivascular nerve and sensory neurotransmitter dysfunction in inflammatory bowel disease. Am J Physiol Heart Circ Physiol 320 H1887-H1902 PMID: 33710922
Christina T et al (2020) nNOS-expressing interneurons control basal and behaviorally evoked arterial dilation in somatosensory cortex of mice. Elife 9 PMID: 33016877
Suyun et al (2020) N-benzhydryl quinuclidine compounds are a potent and Src kinase-independent inhibitor of NALCN channels. Br J Pharmacol 177 3795-3810 PMID: 32436268
Yin et al (2018) Crystal structure of the human NK1 tachykinin receptor. Proc.Natl.Acad.Sci.U.S.A. 115 13264 PMID: 30538204
Sheahan et al (2020) The neurokinin-1 receptor is expressed with gastrin-releasing peptide receptor in spinal interneurons and modulates itch. J.Neurosci 40 8816 PMID: 33051347
Do you know of a great paper that uses CP 99994 dihydrochloride from Tocris? Please let us know.
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