AMG-9810
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MedKoo CAT#: 524224

CAS#: 545395-94-6

Description: AMG 9810 is a competitive antagonist of capsaicin activation of the vanilloid receptor 1 (TRPV1). Additionally, it has been shown to compete with other modes of TRPV1 activation, including proton, heat, and the endogenous ligands: anandamide, N-arachidonyl dopamine and oleoyldopamine.


Price and Availability

Size Price Shipping out time Quantity
100mg USD 550 2 Weeks
200mg USD 950 2 Weeks
500mg USD 1650 2 Weeks
1g USD 2950 2 Weeks
2g USD 4950 2 Weeks
5g USD 7650 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-20. Prices are subject to change without notice.

AMG-9810, 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#: 524224
Name: AMG-9810
CAS#: 545395-94-6
Chemical Formula: C21H23NO3
Exact Mass: 337.16779
Molecular Weight: 337.41
Elemental Analysis: C, 74.75; H, 6.87; N, 4.15; O, 14.23


Synonym: AMG-9810; AMG9810; AMG 9810.

IUPAC/Chemical Name: 3-(4-t-Butylphenyl)-N-(2,3-dihydrobenzo(b)(1,4)dioxin-6-yl)acrylamide

InChi Key: GZTFUVZVLYUPRG-IZZDOVSWSA-N

InChi Code: InChI=1S/C21H23NO3/c1-21(2,3)16-7-4-15(5-8-16)6-11-20(23)22-17-9-10-18-19(14-17)25-13-12-24-18/h4-11,14H,12-13H2,1-3H3,(H,22,23)/b11-6+

SMILES Code: CC(C)(C)c1ccc(cc1)/C=C/C(=O)Nc2ccc3c(c2)OCCO3


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, not in water

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).

HS Tariff Code:
2934.99.9001


References

1: Xu XX, Cao Y, Ding TT, Fu KY, Li Y, Xie QF. Role of TRPV1 and ASIC3 channels in experimental occlusal interference-induced hyperalgesia in rat masseter muscle. Eur J Pain. 2016 Apr;20(4):552-63. doi: 10.1002/ejp.758. Epub 2015 Jul 22. PubMed PMID: 26201614.

2: Alawi KM, Aubdool AA, Liang L, Wilde E, Vepa A, Psefteli MP, Brain SD, Keeble JE. The sympathetic nervous system is controlled by transient receptor potential vanilloid 1 in the regulation of body temperature. FASEB J. 2015 Oct;29(10):4285-98. doi: 10.1096/fj.15-272526. Epub 2015 Jul 1. PubMed PMID: 26136480; PubMed Central PMCID: PMC4650996.

3: Qiao H, Gao Y, Zhang C, Zhou H. Increased expression of TRPV1 in the trigeminal ganglion is involved in orofacial pain during experimental tooth movement in rats. Eur J Oral Sci. 2015 Feb;123(1):17-23. doi: 10.1111/eos.12158. Epub 2014 Nov 19. PubMed PMID: 25407056.

4: Clifton HL, Inceoglu B, Ma L, Zheng J, Schaefer S. TRPV1 channels are involved in niacin-induced cutaneous vasodilation in mice. J Cardiovasc Pharmacol. 2015 Feb;65(2):184-91. doi: 10.1097/FJC.0000000000000181. PubMed PMID: 25387247.

5: Yu X, Hu Y, Yu S. Effects of acid on vagal nociceptive afferent subtypes in guinea pig esophagus. Am J Physiol Gastrointest Liver Physiol. 2014 Aug 15;307(4):G471-8. doi: 10.1152/ajpgi.00156.2014. Epub 2014 Jul 3. PubMed PMID: 24994852; PubMed Central PMCID: PMC4137112.

6: Amiresmaili S, Shamsizadeh A, Allahtavakoli M, Pourshanazari AA, Roohbakhsh A. The effect of intra-ventral hippocampus administration of TRPV1 agonist and antagonist on spatial learning and memory in male rats. Pharmacol Rep. 2014 Feb;66(1):10-4. doi: 10.1016/j.pharep.2013.06.002. Epub 2014 Jan 30. PubMed PMID: 24905300.

7: Hu Y, Liu Z, Yu X, Pasricha PJ, Undem BJ, Yu S. Increased acid responsiveness in vagal sensory neurons in a guinea pig model of eosinophilic esophagitis. Am J Physiol Gastrointest Liver Physiol. 2014 Jul 15;307(2):G149-57. doi: 10.1152/ajpgi.00097.2014. Epub 2014 May 29. PubMed PMID: 24875100; PubMed Central PMCID: PMC4101676.

8: Liu MG, Zhuo M. No requirement of TRPV1 in long-term potentiation or long-term depression in the anterior cingulate cortex. Mol Brain. 2014 Apr 5;7:27. doi: 10.1186/1756-6606-7-27. PubMed PMID: 24708859; PubMed Central PMCID: PMC4234987.

9: Yang F, Guo J, Sun WL, Liu FY, Cai J, Xing GG, Wan Y. The induction of long-term potentiation in spinal dorsal horn after peripheral nociceptive stimulation and contribution of spinal TRPV1 in rats. Neuroscience. 2014 Jun 6;269:59-66. doi: 10.1016/j.neuroscience.2014.03.037. Epub 2014 Mar 26. PubMed PMID: 24680883.

10: Shirazi M, Izadi M, Amin M, Rezvani ME, Roohbakhsh A, Shamsizadeh A. Involvement of central TRPV1 receptors in pentylenetetrazole and amygdala-induced kindling in male rats. Neurol Sci. 2014 Aug;35(8):1235-41. doi: 10.1007/s10072-014-1689-5. Epub 2014 Feb 28. PubMed PMID: 24577898.

11: Robertson S, Thomson AL, Carter R, Stott HR, Shaw CA, Hadoke PW, Newby DE, Miller MR, Gray GA. Pulmonary diesel particulate increases susceptibility to myocardial ischemia/reperfusion injury via activation of sensory TRPV1 and β1 adrenoreceptors. Part Fibre Toxicol. 2014 Feb 25;11:12. doi: 10.1186/1743-8977-11-12. PubMed PMID: 24568236; PubMed Central PMCID: PMC4016506.

12: Kwon SG, Roh DH, Yoon SY, Moon JY, Choi SR, Choi HS, Kang SY, Han HJ, Beitz AJ, Oh SB, Lee JH. Acid evoked thermal hyperalgesia involves peripheral P2Y1 receptor mediated TRPV1 phosphorylation in a rodent model of thrombus induced ischemic pain. Mol Pain. 2014 Jan 9;10:2. doi: 10.1186/1744-8069-10-2. PubMed PMID: 24401144; PubMed Central PMCID: PMC3895685.

13: Vigna SR, Shahid RA, Liddle RA. Ethanol contributes to neurogenic pancreatitis by activation of TRPV1. FASEB J. 2014 Feb;28(2):891-6. doi: 10.1096/fj.13-236208. Epub 2013 Nov 12. PubMed PMID: 24221085; PubMed Central PMCID: PMC3898649.

14: Montrucchio DP, Córdova MM, Santos AR. Plant derived aporphinic alkaloid S-(+)-dicentrine induces antinociceptive effect in both acute and chronic inflammatory pain models: evidence for a role of TRPA1 channels. PLoS One. 2013 Jul 4;8(7):e67730. doi: 10.1371/journal.pone.0067730. Print 2013. PubMed PMID: 23861794; PubMed Central PMCID: PMC3701576.

15: Hakimizadeh E, Oryan S, Hajizadeh Moghaddam A, Shamsizadeh A, Roohbakhsh A. Endocannabinoid System and TRPV1 Receptors in the Dorsal Hippocampus of the Rats Modulate Anxiety-like Behaviors. Iran J Basic Med Sci. 2012 May;15(3):795-802. PubMed PMID: 23493622; PubMed Central PMCID: PMC3586900.

16: Bromberg Z, Goloubinoff P, Saidi Y, Weiss YG. The membrane-associated transient receptor potential vanilloid channel is the central heat shock receptor controlling the cellular heat shock response in epithelial cells. PLoS One. 2013;8(2):e57149. doi: 10.1371/journal.pone.0057149. Epub 2013 Feb 27. PubMed PMID: 23468922; PubMed Central PMCID: PMC3584136.

17: Fernandes VS, Ribeiro AS, Barahona MV, Orensanz LM, Martínez-Sáenz A, Recio P, Martínez AC, Bustamante S, Carballido J, García-Sacristán A, Prieto D, Hernández M. Hydrogen sulfide mediated inhibitory neurotransmission to the pig bladder neck: role of KATP channels, sensory nerves and calcium signaling. J Urol. 2013 Aug;190(2):746-56. doi: 10.1016/j.juro.2013.02.103. Epub 2013 Feb 28. PubMed PMID: 23454157.

18: Razavinasab M, Shamsizadeh A, Shabani M, Nazeri M, Allahtavakoli M, Asadi-Shekaari M, Esmaeli-Mahani S, Sheibani V. Pharmacological blockade of TRPV1 receptors modulates the effects of 6-OHDA on motor and cognitive functions in a rat model of Parkinson's disease. Fundam Clin Pharmacol. 2013 Dec;27(6):632-40. doi: 10.1111/fcp.12015. Epub 2012 Dec 5. PubMed PMID: 23216087.

19: Saloman JL, Chung MK, Ro JY. P2X₃ and TRPV1 functionally interact and mediate sensitization of trigeminal sensory neurons. Neuroscience. 2013 Mar 1;232:226-38. doi: 10.1016/j.neuroscience.2012.11.015. Epub 2012 Nov 29. PubMed PMID: 23201260; PubMed Central PMCID: PMC3600407.

20: Bouyer PG, Tang X, Weber CR, Shen L, Turner JR, Matthews JB. Capsaicin induces NKCC1 internalization and inhibits chloride secretion in colonic epithelial cells independently of TRPV1. Am J Physiol Gastrointest Liver Physiol. 2013 Jan 15;304(2):G142-56. doi: 10.1152/ajpgi.00483.2011. Epub 2012 Nov 8. PubMed PMID: 23139219; PubMed Central PMCID: PMC3543646.