HC-067047
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 530432

CAS#: 883031-03-6

Description: HC-067047 is a potent and selective TRPV4 antagonist. HC-067047 increases functional bladder capacity and reduces micturition frequency in WT mice and rats with cystitis. HC-067047 did not affect bladder function in Trpv4(-/-) mice, demonstrating that its in vivo effects are on target. HC-067047 may provide a promising means of treating bladder


Price and Availability

Size
Price

5mg
USD 230
Size
Price

25mg
USD 580
Size
Price

HC-067047, 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#: 530432
Name: HC-067047
CAS#: 883031-03-6
Chemical Formula: C26H28F3N3O2
Exact Mass: 471.2134
Molecular Weight: 471.5242
Elemental Analysis: C, 66.23; H, 5.99; F, 12.09; N, 8.91; O, 6.79


Synonym: HC-067047; HC 067047; HC067047.

IUPAC/Chemical Name: 2-Methyl-1-[3-(4-morpholinyl)propyl]-5-phenyl-N-[3-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide

InChi Key: NCZYSQOTAYFTNM-UHFFFAOYSA-N

InChi Code: InChI=1S/C26H28F3N3O2/c1-19-23(25(33)30-22-10-5-9-21(17-22)26(27,28)29)18-24(20-7-3-2-4-8-20)32(19)12-6-11-31-13-15-34-16-14-31/h2-5,7-10,17-18H,6,11-16H2,1H3,(H,30,33)

SMILES Code: O=C(C1=C(C)N(CCCN2CCOCC2)C(C3=CC=CC=C3)=C1)NC4=CC=CC(C(F)(F)F)=C4


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: Seki T, Goto K, Kiyohara K, Kansui Y, Murakami N, Haga Y, Ohtsubo T, Matsumura K, Kitazono T. Downregulation of Endothelial Transient Receptor Potential Vanilloid Type 4 Channel and Small-Conductance of Ca2+-Activated K+ Channels Underpins Impaired Endothelium-Dependent Hyperpolarization in Hypertension. Hypertension. 2017 Jan;69(1):143-153. PubMed PMID: 27872234.

2: Hong Z, Tian Y, Yuan Y, Qi M, Li Y, Du Y, Chen L, Chen L. Enhanced Oxidative Stress Is Responsible for TRPV4-Induced Neurotoxicity. Front Cell Neurosci. 2016 Oct 17;10:232. PubMed PMID: 27799895; PubMed Central PMCID: PMC5065954.

3: Isogai A, Lee K, Mitsui R, Hashitani H. Functional coupling of TRPV4 channels and BK channels in regulating spontaneous contractions of the guinea pig urinary bladder. Pflugers Arch. 2016 Sep;468(9):1573-85. doi: 10.1007/s00424-016-1863-0. PubMed PMID: 27497848.

4: Yang F, Zhou L, Wang D, Yang LL, Yuan GR, Huang QY. Suppression of TRPV4 channels ameliorates anti-dipsogenic effects under hypoxia in the subfornical organ of rats. Sci Rep. 2016 Jul 20;6:30168. doi: 10.1038/srep30168. PubMed PMID: 27436489; PubMed Central PMCID: PMC4951807.

5: Sakuta H, Nishihara E, Hiyama TY, Lin CH, Noda M. Nax signaling evoked by an increase in [Na+] in CSF induces water intake via EET-mediated TRPV4 activation. Am J Physiol Regul Integr Comp Physiol. 2016 Aug 1;311(2):R299-306. doi: 10.1152/ajpregu.00352.2015. PubMed PMID: 27252474.

6: Murphy TV, Kanagarajah A, Toemoe S, Bertrand PP, Grayson TH, Britton FC, Leader L, Senadheera S, Sandow SL. TRPV3 expression and vasodilator function in isolated uterine radial arteries from non-pregnant and pregnant rats. Vascul Pharmacol. 2016 Aug;83:66-77. doi: 10.1016/j.vph.2016.04.004. PubMed PMID: 27073026.

7: Zhang LP, Kline RH 4th, Deevska G, Ma F, Nikolova-Karakashian M, Westlund KN. Alcohol and high fat induced chronic pancreatitis: TRPV4 antagonist reduces hypersensitivity. Neuroscience. 2015 Dec 17;311:166-79. doi: 10.1016/j.neuroscience.2015.10.028. PubMed PMID: 26480812; PubMed Central PMCID: PMC4670827.

8: Jo AO, Ryskamp DA, Phuong TT, Verkman AS, Yarishkin O, MacAulay N, Križaj D. TRPV4 and AQP4 Channels Synergistically Regulate Cell Volume and Calcium Homeostasis in Retinal Müller Glia. J Neurosci. 2015 Sep 30;35(39):13525-37. doi: 10.1523/JNEUROSCI.1987-15.2015. PubMed PMID: 26424896; PubMed Central PMCID: PMC4588615.

9: Sánchez JC, Rivera RA, Muñoz LV. TRPV4 Channels in Human White Adipocytes: Electrophysiological Characterization and Regulation by Insulin. J Cell Physiol. 2016 Apr;231(4):954-63. doi: 10.1002/jcp.25187. PubMed PMID: 26381274.

10: Shahidullah M, Mandal A, Delamere NA. Damage to lens fiber cells causes TRPV4-dependent Src family kinase activation in the epithelium. Exp Eye Res. 2015 Nov;140:85-93. doi: 10.1016/j.exer.2015.08.013. PubMed PMID: 26318609; PubMed Central PMCID: PMC4763713.

11: Yin J, Michalick L, Tang C, Tabuchi A, Goldenberg N, Dan Q, Awwad K, Wang L, Erfinanda L, Nouailles G, Witzenrath M, Vogelzang A, Lv L, Lee WL, Zhang H, Rotstein O, Kapus A, Szaszi K, Fleming I, Liedtke WB, Kuppe H, Kuebler WM. Role of Transient Receptor Potential Vanilloid 4 in Neutrophil Activation and Acute Lung Injury. Am J Respir Cell Mol Biol. 2016 Mar;54(3):370-83. doi: 10.1165/rcmb.2014-0225OC. PubMed PMID: 26222277.

12: Zou Q, Leung SW, Vanhoutte PM. Transient Receptor Potential Channel Opening Releases Endogenous Acetylcholine, which Contributes to Endothelium-Dependent Relaxation Induced by Mild Hypothermia in Spontaneously Hypertensive Rat but Not Wistar-Kyoto Rat Arteries. J Pharmacol Exp Ther. 2015 Aug;354(2):121-30. doi: 10.1124/jpet.115.223693. PubMed PMID: 26060231.

13: Jie P, Hong Z, Tian Y, Li Y, Lin L, Zhou L, Du Y, Chen L, Chen L. Activation of transient receptor potential vanilloid 4 induces apoptosis in hippocampus through downregulating PI3K/Akt and upregulating p38 MAPK signaling pathways. Cell Death Dis. 2015 Jun 4;6:e1775. doi: 10.1038/cddis.2015.146. PubMed PMID: 26043075; PubMed Central PMCID: PMC4669828.

14: Nayak PS, Wang Y, Najrana T, Priolo LM, Rios M, Shaw SK, Sanchez-Esteban J. Mechanotransduction via TRPV4 regulates inflammation and differentiation in fetal mouse distal lung epithelial cells. Respir Res. 2015 May 27;16:60. doi: 10.1186/s12931-015-0224-4. PubMed PMID: 26006045; PubMed Central PMCID: PMC4446903.

15: Jie P, Tian Y, Hong Z, Li L, Zhou L, Chen L, Chen L. Blockage of transient receptor potential vanilloid 4 inhibits brain edema in middle cerebral artery occlusion mice. Front Cell Neurosci. 2015 Apr 10;9:141. doi: 10.3389/fncel.2015.00141. PubMed PMID: 25914628; PubMed Central PMCID: PMC4392311.

16: Peixoto-Neves D, Wang Q, Leal-Cardoso JH, Rossoni LV, Jaggar JH. Eugenol dilates mesenteric arteries and reduces systemic BP by activating endothelial cell TRPV4 channels. Br J Pharmacol. 2015 Jul;172(14):3484-94. doi: 10.1111/bph.13156. PubMed PMID: 25832173; PubMed Central PMCID: PMC4507154.

17: Vizin RC, Scarpellini Cda S, Ishikawa DT, Correa GM, de Souza CO, Gargaglioni LH, Carrettiero DC, Bícego KC, Almeida MC. TRPV4 activates autonomic and behavioural warmth-defence responses in Wistar rats. Acta Physiol (Oxf). 2015 Jun;214(2):275-89. doi: 10.1111/apha.12477. PubMed PMID: 25739906.

18: Zhao PY, Gan G, Peng S, Wang SB, Chen B, Adelman RA, Rizzolo LJ. TRP Channels Localize to Subdomains of the Apical Plasma Membrane in Human Fetal Retinal Pigment Epithelium. Invest Ophthalmol Vis Sci. 2015 Mar 3;56(3):1916-23. doi: 10.1167/iovs.14-15738. PubMed PMID: 25736794; PubMed Central PMCID: PMC4364639.

19: Son GY, Yang YM, Park WS, Chang I, Shin DM. Hypotonic stress induces RANKL via transient receptor potential melastatin 3 (TRPM3) and vaniloid 4 (TRPV4) in human PDL cells. J Dent Res. 2015 Mar;94(3):473-81. doi: 10.1177/0022034514567196. PubMed PMID: 25595364; PubMed Central PMCID: PMC4814022.

20: Sánchez JC, López-Zapata DF, Wilkins RJ. TRPV4 channels activity in bovine articular chondrocytes: regulation by obesity-associated mediators. Cell Calcium. 2014 Dec;56(6):493-503. doi: 10.1016/j.ceca.2014.10.006. PubMed PMID: 25459300.