CP-376395 free base
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MedKoo CAT#: 555143

CAS#: 175140-00-8 (free base)

Description: CP-376395 is a CRF1-selective antagonist. CRF1 receptor signaling regulates food and fluid intake in the drinking-in-the-dark model of binge alcohol consumption


Price and Availability

Size
Price

200mg
USD 1650
2g
USD 4950
Size
Price

500mg
USD 2250
5g
USD 8650
Size
Price

1g
USD 3650

CP-376395 free base, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 555143
Name: CP-376395 free base
CAS#: 175140-00-8 (free base)
Chemical Formula: C20H28N2O
Exact Mass: 312.2202
Molecular Weight: 312.457
Elemental Analysis: C, 76.88; H, 9.03; N, 8.97; O, 5.12


Related CAS #: 1013933-37-3 (HCl)   175140-00-8 (free base)    

Synonym: CP-376395; CP 376395; CP376395; CP-376,395; CP 376,395; CP376,395.

IUPAC/Chemical Name: N,N-diethyl-2-(mesityloxy)-3,6-dimethylpyridin-4-amine

InChi Key: PRHLXIOMJCBPHZ-UHFFFAOYSA-N

InChi Code: InChI=1S/C20H28N2O/c1-8-22(9-2)18-12-16(6)21-20(17(18)7)23-19-14(4)10-13(3)11-15(19)5/h10-12H,8-9H2,1-7H3

SMILES Code: CCN(CC)C1=C(C)C(OC2=C(C)C=C(C)C=C2C)=NC(C)=C1


Technical Data

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

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).

Harmonized System Code:
293490


References

1: Residues remote from the binding pocket control the antagonist selectivity towards the corticotropin-releasing factor receptor-1 Xianqiang Sun, Jianxin Cheng, Xu Wang, Yun Tang, Hans Ågren, Yaoquan Tu Sci Rep. 2015; 5: 8066. Published online 2015 Jan 28. doi: 10.1038/srep08066 PMCID: PMC4308710

2: Conformational thermostabilisation of corticotropin releasing factor receptor 1 James Kean, Andrea Bortolato, Kaspar Hollenstein, Fiona H. Marshall, Ali Jazayeri Sci Rep. 2015; 5: 11954. Published online 2015 Jul 10. doi: 10.1038/srep11954 PMCID: PMC4498186

3: Aversive stimuli drive drug seeking in a state of low dopamine tone Robert C. Twining, Daniel S. Wheeler, Amanda L. Ebben, Andre J. Jacobsen, Mykel A. Robble, John R. Mantsch, Robert A. Wheeler Biol Psychiatry. Author manuscript; available in PMC 2016 May 15.Published in final edited form as: Biol Psychiatry. 2015 May 15; 77(10): 895–902. Published online 2014 Sep 22. doi: 10.1016/j.biopsych.2014.09.004 PMCID: PMC4369463

4: Augmented Cocaine Seeking in Response to Stress or CRF Delivered into the Ventral Tegmental Area Following Long-Access Self-Administration is Mediated by CRF-R1 but not CRF-R2 Receptors Jordan M. Blacktop, Chad Seubert, David A. Baker, Nathan Ferda, Geng Lee, Evan N. Graf, John R. Mantsch J Neurosci. Author manuscript; available in PMC 2012 Sep 23.Published in final edited form as: J Neurosci. 2011 Aug 3; 31(31): 11396–11403. doi: 10.1523/JNEUROSCI.1393-11.2011 PMCID: PMC3449095

5: Dissociation of mu opioid receptor and CRF-R1 antagonist effects on escalated ethanol consumption and mPFC serotonin in C57BL/6J mice Lara S. Hwa, Akiko Shimamoto, Tala Kayyali, Kevin J. Norman, Rita J. Valentino, Joseph F. DeBold, Klaus A. Miczek Addict Biol. Author manuscript; available in PMC 2017 Jan 1.Published in final edited form as: Addict Biol. 2016 Jan; 21(1): 111–124. Published online 2014 Sep 28. doi: 10.1111/adb.12189 PMCID: PMC4377124

6: Decoding Corticotropin-Releasing Factor Receptor Type 1 Crystal Structures Andrew S. Doré, Andrea Bortolato, Kaspar Hollenstein, Robert K.Y. Cheng, Randy J. Read, Fiona H. Marshall Curr Mol Pharmacol. 2017 Nov; 10(4): 334–344. Published online 2017 Nov. doi: 10.2174/1874467210666170110114727 PMCID: PMC5684783

7: Importance of CRF Receptor-Mediated Mechanisms of the Bed Nucleus of the Stria Terminalis in the Processing of Anxiety and Pain Lee Tran, Jay Schulkin, Beverley Greenwood-Van Meerveld Neuropsychopharmacology. 2014 Oct; 39(11): 2633–2645. Prepublished online 2014 May 23. Published online 2014 Jun 18. doi: 10.1038/npp.2014.117 PMCID: PMC4207343

8: Social Stress and CRF–Dopamine Interactions in the VTA: Role in Long-Term Escalation of Cocaine Self-Administration Christopher O. Boyson, Elizabeth N. Holly, Akiko Shimamoto, Lucas Albrechet-Souza, Lindsay A. Weiner, Joseph F. DeBold, Klaus A. Miczek J Neurosci. 2014 May 7; 34(19): 6659–6667. doi: 10.1523/JNEUROSCI.3942-13.2014 PMCID: PMC4012317

9: CRF1 receptor signaling regulates food and fluid intake in the drinking-in-the-dark model of binge alcohol consumption William J. Giardino, Andrey E. Ryabinin Alcohol Clin Exp Res. Author manuscript; available in PMC 2014 Jul 1.Published in final edited form as: Alcohol Clin Exp Res. 2013 Jul; 37(7): 1161–1170. Published online 2013 Feb 7. doi: 10.1111/acer.12076 PMCID: PMC3657581

10: Anxiogenic effects of CGRP within the BNST may be mediated by CRF acting at BNST CRFR1 receptors KS Sink, A Chung, KJ Ressler, M Davis, DL Walker Behav Brain Res. Author manuscript; available in PMC 2014 Apr 15.Published in final edited form as: Behav Brain Res. 2013 Apr 15; 243: 286–293. Published online 2013 Feb 1. doi: 10.1016/j.bbr.2013.01.024 PMCID: PMC3593796

11: Dissociation of corticotropin-releasing factor receptor subtype involvement in sensitivity to locomotor effects of methamphetamine and cocaine William J. Giardino, Gregory P. Mark, Mary P. Stenzel-Poore, Andrey E. Ryabinin Psychopharmacology (Berl) Author manuscript; available in PMC 2012 Feb 1.Published in final edited form as: Psychopharmacology (Berl). 2012 Feb; 219(4): 1055–1063. Published online 2011 Aug 11. doi: 10.1007/s00213-011-2433-y PMCID: PMC3266955

12: Rosetta Broker for membrane protein structure prediction: concentrative nucleoside transporter 3 and corticotropin-releasing factor receptor 1 test cases Dorota Latek BMC Struct Biol. 2017; 17: 8. Published online 2017 Aug 3. doi: 10.1186/s12900-017-0078-8 PMCID: PMC5543540

13: Structure of Class B GPCRs: new horizons for drug discovery Andrea Bortolato, Andrew S Doré, Kaspar Hollenstein, Benjamin G Tehan, Jonathan S Mason, Fiona H Marshall Br J Pharmacol. 2014 Jul; 171(13): 3132–3145. Published online 2014 Jun 10. doi: 10.1111/bph.12689 PMCID: PMC4080969

14: Adaptive simulations, towards interactive protein-ligand modeling Daniel Lecina, Joan F. Gilabert, Victor Guallar Sci Rep. 2017; 7: 8466. Published online 2017 Aug 16. doi: 10.1038/s41598-017-08445-5 PMCID: PMC5559483

15: Insights into the structure of class B GPCRs Kaspar Hollenstein, Chris de Graaf, Andrea Bortolato, Ming-Wei Wang, Fiona H. Marshall, Raymond C. Stevens Trends Pharmacol Sci. Author manuscript; available in PMC 2015 Jan 1.Published in final edited form as: Trends Pharmacol Sci. 2014 Jan; 35(1): 12–22. Published online 2013 Dec 18. doi: 10.1016/j.tips.2013.11.001 PMCID: PMC3931419

16: Transmembrane signal transduction by peptide hormones via family B G protein-coupled receptors Kelly J. Culhane, Yuting Liu, Yingying Cai, Elsa C. Y. Yan Front Pharmacol. 2015; 6: 264. Published online 2015 Nov 5. doi: 10.3389/fphar.2015.00264 PMCID: PMC4633518

17: Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders P. Jeffrey Conn, Craig W. Lindsley, Jens Meiler, Colleen M. Niswender Nat Rev Drug Discov. Author manuscript; available in PMC 2015 Mar 1.Published in final edited form as: Nat Rev Drug Discov. 2014 Sep; 13(9): 692–708. doi: 10.1038/nrd4308 PMCID: PMC4208620

18: Importance of Stress Receptor-Mediated Mechanisms in the Amygdala on Visceral Pain Perception in an Intrinsically Anxious Rat Anthony C. Johnson, Lee Tran, Jay Schulkin, Beverley Greenwood-Van Meerveld Neurogastroenterol Motil. Author manuscript; available in PMC 2013 May 1.Published in final edited form as: Neurogastroenterol Motil. 2012 May; 24(5): 479–e219. Published online 2012 Feb 26. doi: 10.1111/j.1365-2982.2012.01899.x PMCID: PMC3461498

19: New paradigms in GPCR drug discovery Kenneth A. Jacobson Biochem Pharmacol. Author manuscript; available in PMC 2016 Dec 15.Published in final edited form as: Biochem Pharmacol. 2015 Dec 15; 98(4): 541–555. Published online 2015 Aug 8. doi: 10.1016/j.bcp.2015.08.085 PMCID: PMC4967540

20: Structural-Functional Analysis of the Third Transmembrane Domain of the Corticotropin-releasing Factor Type 1 Receptor: ROLE IN ACTIVATION AND ALLOSTERIC ANTAGONISM Katerina Spyridaki, Minos-Timotheos Matsoukas, Arnau Cordomi, Kostas Gkountelias, Maria Papadokostaki, Thomas Mavromoustakos, Diomedes E. Logothetis, Andrew N. Margioris, Leonardo Pardo, George Liapakis J Biol Chem. 2014 Jul 4; 289(27): 18966–18977. Published online 2014 May 16. doi: 10.1074/jbc.M113.544460 PMCID: PMC4081936