RN9893 | CAS#1803003-68-0 | TRPV4 receptor antagonist

RN9893
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 561416

CAS#: 1803003-68-0 (free base)

Description: RN-9893 is a potent and selective antagonist of the Transient Receptor Potential ion channel TRPV4. RN-9893 has IC50 values of 420 nM, 660 nM, and 320 nM for human, rat and mouse TRPV4 receptors, respectively. RN-9893 shows excellent selectivity over related TRP receptors with no inhibition of TRPV1 at a concentration of 10 μM, an IC50 >30 μM against TRPV3, an IC50 of approximately 30 μM against TRPM8, and also good selectivity using 54 binding assays against common biological targets.

Chemical Structure

RN9893

CAS# 1803003-68-0 (free base)

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 561416
Name: RN9893
CAS#: 1803003-68-0 (free base)
Chemical Formula: C21H23F3N4O5S
Exact Mass: 500.13
Molecular Weight: 500.490
Elemental Analysis: C, 50.40; H, 4.63; F, 11.39; N, 11.19; O, 15.98; S, 6.41

Price and Availability

Size	Price	Availability
25mg	USD 250	2 Weeks
50mg	USD 450	2 Weeks
100mg	USD 750	2 Weeks
200mg	USD 1250	2 Weeks
500mg	USD 2650	2 Weeks
1g	USD 3850	2 Weeks
2g	USD 6450	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Related CAS #: 2109450-40-8 (HCl) 1803003-68-0 (free base)

Synonym: RN9893; RN-9893; RN 9893;

IUPAC/Chemical Name: N-(4-((4-Isopropylpiperazin-1-yl)sulfonyl)phenyl)-2-nitro-4-(trifluoromethyl)benzamide

InChi Key: KORKKQLDGMHNKO-UHFFFAOYSA-N

InChi Code: 1S/C21H23F3N4O5S/c1-14(2)26-9-11-27(12-10-26)34(32,33)17-6-4-16(5-7-17)25-20(29)18-8-3-15(21(22,23)24)13-19(18)28(30)31/h3-8,13-14H,9-12H2,1-2H3,(H,25,29)

SMILES Code: O=C(NC1=CC=C(S(=O)(N2CCN(C(C)C)CC2)=O)C=C1)C3=CC=C(C(F)(F)F)C=C3[N+]([O-])=O

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:

Product Data:

Product Data

Instruction:

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Biological target:	RN-9893 has IC50 values of 420 nM, 660 nM, and 320 nM for human, rat and mouse TRPV4 receptors, respectively. RN-9893 shows >15-fold selectivity for TRPV4 over TRPV1, TRPV3 and TRPM8 receptors with no inhibition of TRPV1 at a concentration of 10 μM, an IC50 >30 μM against TRPV3, an IC50 of approximately 30 μM against TRPM8, and also good selectivity using 54 binding assays against common biological targets.
In vitro activity:	Cyclic stretch-induced expression of COL I mRNA in cultured VICFB was blocked by RN-9893 while having no effect on the stretch-induced expression of COL III. Reference: PLoS One. 2020 Oct 15;15(10):e0240532. https://pubmed.ncbi.nlm.nih.gov/33057457/
In vivo activity:	RN-9893 26, inhibited human, rat and murine variants of TRPV4, and showed excellent selectivity over related TRP receptors, such as TRPV1, TRPV3 and TRPM8. The overall profile for RN-9893 indicates its possible use as a probe for in vivo applications. Reference: Bioorg Med Chem Lett. 2015 Sep 15;25(18):4011-5. https://pubmed.ncbi.nlm.nih.gov/26235950/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	25.0	49.95

Preparing Stock Solutions

The following data is based on the product molecular weight 500.49 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

Formulation protocol:	1. Al-Shammari H, Latif N, Sarathchandra P, McCormack A, Rog-Zielinska EA, Raja S, Kohl P, Yacoub MH, Peyronnet R, Chester AH. Expression and function of mechanosensitive ion channels in human valve interstitial cells. PLoS One. 2020 Oct 15;15(10):e0240532. doi: 10.1371/journal.pone.0240532. PMID: 33057457; PMCID: PMC7561104. 2. Wei ZL, Nguyen MT, O'Mahony DJ, Acevedo A, Zipfel S, Zhang Q, Liu L, Dourado M, Chi C, Yip V, DeFalco J, Gustafson A, Emerling DE, Kelly MG, Kincaid J, Vincent F, Duncton MA. Identification of orally-bioavailable antagonists of the TRPV4 ion-channel. Bioorg Med Chem Lett. 2015 Sep 15;25(18):4011-5. doi: 10.1016/j.bmcl.2015.06.098. Epub 2015 Jul 6. PMID: 26235950.
In vitro protocol:	1. Al-Shammari H, Latif N, Sarathchandra P, McCormack A, Rog-Zielinska EA, Raja S, Kohl P, Yacoub MH, Peyronnet R, Chester AH. Expression and function of mechanosensitive ion channels in human valve interstitial cells. PLoS One. 2020 Oct 15;15(10):e0240532. doi: 10.1371/journal.pone.0240532. PMID: 33057457; PMCID: PMC7561104.
In vivo protocol:	1. Wei ZL, Nguyen MT, O'Mahony DJ, Acevedo A, Zipfel S, Zhang Q, Liu L, Dourado M, Chi C, Yip V, DeFalco J, Gustafson A, Emerling DE, Kelly MG, Kincaid J, Vincent F, Duncton MA. Identification of orally-bioavailable antagonists of the TRPV4 ion-channel. Bioorg Med Chem Lett. 2015 Sep 15;25(18):4011-5. doi: 10.1016/j.bmcl.2015.06.098. Epub 2015 Jul 6. PMID: 26235950.

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1. Al-Shammari H, Latif N, Sarathchandra P, McCormack A, Rog-Zielinska EA, Raja S, Kohl P, Yacoub MH, Peyronnet R, Chester AH. Expression and function of mechanosensitive ion channels in human valve interstitial cells. PLoS One. 2020 Oct 15;15(10):e0240532. doi: 10.1371/journal.pone.0240532. PMID: 33057457; PMCID: PMC7561104.

2. Wei ZL, Nguyen MT, O'Mahony DJ, Acevedo A, Zipfel S, Zhang Q, Liu L, Dourado M, Chi C, Yip V, DeFalco J, Gustafson A, Emerling DE, Kelly MG, Kincaid J, Vincent F, Duncton MA. Identification of orally-bioavailable antagonists of the TRPV4 ion-channel. Bioorg Med Chem Lett. 2015 Sep 15;25(18):4011-5. doi: 10.1016/j.bmcl.2015.06.098. Epub 2015 Jul 6. PMID: 26235950.

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