RS-100329 | CAS#1215654-26-4 | α1A-adrenoceptor antagonist

MedKoo Cat#: 532581 | Name: RS 100329 HCl

Description:

WARNING: This product is for research use only, not for human or veterinary use.

RS 100329 is a subtype-selective α1A-adrenoceptor antagonist (pKi = 9.6 for human cloned α1A receptors). RS 100329 displays 126- and 50-fold selectivity over human α1B and α1D receptors respectively.

Chemical Structure

RS 100329 HCl

CAS#215654-26-4 (HCl)

Theoretical Analysis

MedKoo Cat#: 532581

Name: RS 100329 HCl

CAS#: 215654-26-4 (HCl)

Chemical Formula: C20H26ClF3N4O3

Exact Mass: 462.1646

Molecular Weight: 462.90

Elemental Analysis: C, 51.89; H, 5.66; Cl, 7.66; F, 12.31; N, 12.10; O, 10.37

Price and Availability

Size	Price	Availability
50mg	USD 750.00	2 Weeks
100mg	USD 1,250.00	2 Weeks
200mg	USD 1,950.00	2 Weeks
500mg	USD 2,950.00	2 Weeks
1g	USD 4,350.00	2 Weeks
2g	USD 7,450.00	2 Weeks

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Related CAS #

232953-52-5 (free base) 215654-26-4 (HCl)

Synonym

RS-100329; RS 100329; RS100329; RS 100329 HCl; RS100329 HCl.

IUPAC/Chemical Name

5-methyl-3-(3-(4-(2-(2,2,2-trifluoroethoxy)phenyl)piperazin-1-yl)propyl)pyrimidine-2,4(1H,3H)-dione hydrochloride

InChi Key

CWVABCXVOAVUJL-UHFFFAOYSA-N

InChi Code

InChI=1S/C20H25F3N4O3.ClH/c1-15-13-24-19(29)27(18(15)28)8-4-7-25-9-11-26(12-10-25)16-5-2-3-6-17(16)30-14-20(21,22)23;/h2-3,5-6,13H,4,7-12,14H2,1H3,(H,24,29);1H

SMILES Code

CC1=CNC(N(C1=O)CCCN2CCN(C3=C(C=CC=C3)OCC(F)(F)F)CC2)=O.Cl

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).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 462.90 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	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Yarotskyy V, Nass SR, Hahn YK, Contois L, McQuiston AR, Knapp PE, Hauser KF. Sustained fentanyl exposure inhibits neuronal activity in dissociated striatal neuronal-glial cocultures through actions independent of opioid receptors. J Neurophysiol. 2024 Sep 1;132(3):1056-1073. doi: 10.1152/jn.00444.2023. Epub 2024 Aug 7. PMID: 39110896; PMCID: PMC11427067. 2: Xie N, Wang F, Chen D, Zhou J, Xu J, Qu F. Immune dysfunction mediated by the competitive endogenous RNA network in fetal side placental tissue of polycystic ovary syndrome. PLoS One. 2024 Mar 21;19(3):e0300461. doi: 10.1371/journal.pone.0300461. PMID: 38512862; PMCID: PMC10956758. 3: Alsufyani HA, Daly C, Docherty JR. Interaction between α1B - and other α1 - and α2 -adrenoceptors in producing contractions of mouse spleen. Basic Clin Pharmacol Toxicol. 2021 Dec;129(6):416-426. doi: 10.1111/bcpt.13639. Epub 2021 Sep 25. PMID: 34383990. 4: Alsufyani HA, McCormick PA, Docherty JR. Both α1B- and α1A-adrenoceptor subtypes are involved in contractions of rat spleen. Pharmacol Rep. 2021 Feb;73(1):255-260. doi: 10.1007/s43440-020-00118-x. Epub 2020 Aug 28. PMID: 32860192. 5: Ishida H, Saito SY, Ishikawa T. α1A-Adrenoceptors, but not α1B- or α1D-adrenoceptors, contribute to enhanced contractile response to phenylephrine in cooling conditions in the rat tail artery. Eur J Pharmacol. 2018 Nov 5;838:120-128. doi: 10.1016/j.ejphar.2018.09.004. Epub 2018 Sep 5. PMID: 30194940. 6: Pacini ESA, Castilho ACS, Hebeler-Barbosa F, Pupo AS, Kiguti LRA. Contraction of Rat Cauda Epididymis Smooth Muscle to α1-Adrenoceptor Activation Is Mediated by α1A-Adrenoceptors. J Pharmacol Exp Ther. 2018 Jul;366(1):21-28. doi: 10.1124/jpet.117.246710. Epub 2018 Apr 23. PMID: 29685886. 7: Ribeiro CA, Pupo AS. Involvement of α1B-adrenoceptors in the anti-immobility effect of imipramine in the tail suspension test. Eur J Pharmacol. 2015 Mar 5;750:39-42. doi: 10.1016/j.ejphar.2015.01.010. Epub 2015 Jan 21. PMID: 25617795. 8: Docherty JR. Prazosin has low potency at α1A-adrenoceptors and high potency at α1D -adrenoceptors in rat vas deferens. Auton Autacoid Pharmacol. 2013 Oct;33(3-4):49-57. doi: 10.1111/aap.12015. Epub 2013 Sep 18. PMID: 24074250. 9: Zacharia J, Mauban JR, Raina H, Fisher SA, Wier WG. High vascular tone of mouse femoral arteries in vivo is determined by sympathetic nerve activity via α1A- and α1D-adrenoceptor subtypes. PLoS One. 2013 Jun 12;8(6):e65969. doi: 10.1371/journal.pone.0065969. PMID: 23776582; PMCID: PMC3680395. 10: Docherty JR. Yohimbine antagonises α1A- and α1D-adrenoceptor mediated components in addition to the α2A-adrenoceptor component to pressor responses in the pithed rat. Eur J Pharmacol. 2012 Mar 15;679(1-3):90-4. doi: 10.1016/j.ejphar.2012.01.001. Epub 2012 Jan 21. PMID: 22290390. 11: López-Islas I, López-Sánchez P, Ibarra M, Gallardo-Ortiz IA, Terrón JA. Effect of inter-renal aortic coarctation-induced hypertension on function and expression of vascular α(1A)- and α(1D)-adrenoceptors. Can J Physiol Pharmacol. 2012 Jan;90(1):1-12. doi: 10.1139/y11-099. Epub 2011 Dec 12. PMID: 22149309. 12: Martínez-Salas SG, Campos-Peralta JM, Pardo JP, Hernández-Muñoz R, Ibarra M, Tanoue A, Tsujimoto G, Villalobos-Molina R. α(1D)-Adrenoceptor regulates the vasopressor action of α(1A)-adrenoceptor in mesenteric vascular bed of α(1D)-adrenoceptor knockout mice. Auton Autacoid Pharmacol. 2011 Jul- Oct;31(3-4):64-71. doi: 10.1111/j.1474-8673.2011.00468.x. PMID: 21951586. 13: Docherty JR. Vasopressor nerve responses in the pithed rat, previously identified as α2-adrenoceptor mediated, may be α1D-adrenoceptor mediated. Eur J Pharmacol. 2011 May 11;658(2-3):182-6. doi: 10.1016/j.ejphar.2011.02.029. Epub 2011 Mar 2. PMID: 21376031. 14: Gómez-Zamudio JH, Villalobos-Molina R. Adventitia removal does not modify the alphaID-adrenoceptors response in aorta during hypertension and ageing. Auton Autacoid Pharmacol. 2009 Jul;29(3):117-33. doi: 10.1111/j.1474-8673.2009.00432.x. PMID: 19566752. 15: Recio P, Orensanz LM, Martínez MP, Navarro-Dorado J, Bustamante S, García- Sacristán A, Prieto D, Hernández M. Noradrenergic vasoconstriction of pig prostatic small arteries. Naunyn Schmiedebergs Arch Pharmacol. 2008 Feb;376(6):397-406. doi: 10.1007/s00210-007-0227-x. Epub 2008 Jan 3. PMID: 18172615. 16: Bexis S, Docherty JR. Role of alpha1-adrenoceptor subtypes in the effects of methylenedioxy methamphetamine (MDMA) on body temperature in the mouse. Br J Pharmacol. 2008 Feb;153(3):591-7. doi: 10.1038/sj.bjp.0707590. Epub 2007 Nov 26. PMID: 18037913; PMCID: PMC2241778. 17: Martínez-Salas SG, Campos-Peralta JM, Pares-Hipolito J, Gallardo-Ortíz IA, Ibarra M, Villalobos-Molina R. Alpha1A-adrenoceptors predominate in the control of blood pressure in mouse mesenteric vascular bed. Auton Autacoid Pharmacol. 2007 Jul;27(3):137-42. doi: 10.1111/j.1474-8673.2007.00403.x. PMID: 17584443. 18: Awe SO, Adeagbo AS. Vascular alpha1-adrenoceptors in isolated perfused rat kidney: influence of ageing. Auton Autacoid Pharmacol. 2007 Jan;27(1):19-26. doi: 10.1111/j.1474-8673.2006.00385.x. PMID: 17199872. 19: Parés-Hipólito J, Gómez-Zamudio JH, Gallardo-Ortiz IA, López-Guerrero JJ, Santamaría-Ortiz J, Ibarra M, Villalobos-Molina R. Selective agonists reveal alpha(1A)- and alpha(1B)-adrenoceptor subtypes in caudal artery of the young rat. Auton Autacoid Pharmacol. 2006 Oct;26(4):371-8. doi: 10.1111/j.1474-8673.2006.00380.x. PMID: 16968476. 20: Bagot K, Chess-Williams R. Alpha(1A/L)-adrenoceptors mediate contraction of the circular smooth muscle of the pig urethra. Auton Autacoid Pharmacol. 2006 Oct;26(4):345-53. doi: 10.1111/j.1474-8673.2006.00374.x. PMID: 16968473.