MedKoo Cat#: 561416 | Name: RN9893
Featured New

Description:

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

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
RN9893
CAS#1803003-68-0 (free base)

Theoretical Analysis

MedKoo Cat#: 561416

Name: RN9893

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

Chemical Formula: C21H23F3N4O5S

Exact Mass: 500.1341

Molecular Weight: 500.49

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 Quantity
25mg USD 250.00 2 Weeks
50mg USD 450.00 2 Weeks
100mg USD 750.00 2 Weeks
200mg USD 1,250.00 2 Weeks
500mg USD 2,650.00 2 Weeks
1g USD 3,850.00 2 Weeks
2g USD 6,450.00 2 Weeks
Show More
Bulk Inquiry
Buy Now
Add to Cart
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
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/
Solvent mg/mL mM comments
Solubility
DMSO 25.0 49.95
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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.

Recalculate based on batch purity %
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.
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. 3: Beddek K, Raffin F, Borgel D, Saller F, Riccobono D, Bobe R, Boittin FX. TRPV4 channel activation induces the transition of venous and arterial endothelial cells toward a pro-inflammatory phenotype. Physiol Rep. 2021 Feb;9(3):e14613. doi: 10.14814/phy2.14613. PMID: 33512067; PMCID: PMC7845413. 4: Wang M, Zhang Y, Cai X, Yang S, Sun S, Zhou S, Lv W, Du N, Li Y, Ma C, Ren K, Liu M, Tang B, Wang A, Chen X, Li P, Lv K, Zheng Z. Exploration and structure-activity relationship research of benzenesulfonamide derivatives as potent TRPV4 inhibitors for treating acute lung injury. Bioorg Chem. 2024 Jun;147:107396. doi: 10.1016/j.bioorg.2024.107396. Epub 2024 Apr 30. PMID: 38705108.