VU0240551
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 532899

CAS#: 893990-34-6

Description: VU0240551 is an inhibitor of the neuronal K-Cl cotransporter, KCC2 (IC50 = 560 nM for K+ uptake assay in KCC2-overexpressing cells). VU0240551 exhibits selectivity over the Na-K-2Cl cotransporter, NKCCl. It also inhibits hERG and L-type Ca2+ channels.


Chemical Structure

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VU0240551
CAS# 893990-34-6

Theoretical Analysis

MedKoo Cat#: 532899
Name: VU0240551
CAS#: 893990-34-6
Chemical Formula: C16H14N4OS2
Exact Mass: 342.0609
Molecular Weight: 342.44
Elemental Analysis: C, 56.12; H, 4.12; N, 16.36; O, 4.67; S, 18.72

Price and Availability

Size Price Availability Quantity
10.0mg USD 290.0 2 Weeks
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Synonym: VU0240551, VU 0240551, VU- 0240551

IUPAC/Chemical Name: N-(4-methyl-1,3-thiazol-2-yl)-2-[(6-phenylpyridazin-3-yl)sulfanyl]acetamide

InChi Key: WJRWSLORVIHRNX-UHFFFAOYSA-N

InChi Code: InChI=1S/C16H14N4OS2/c1-11-9-23-16(17-11)18-14(21)10-22-15-8-7-13(19-20-15)12-5-3-2-4-6-12/h2-9H,10H2,1H3,(H,17,18,21)

SMILES Code: O=C(NC1=NC(C)=CS1)CSC2=NN=C(C3=CC=CC=C3)C=C2

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

Preparing Stock Solutions

The following data is based on the product molecular weight 342.44 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

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1: Gu W, Zhang W, Lei Y, Cui Y, Chu S, Gu X, Ma Z. Activation of spinal alpha-7 nicotinic acetylcholine receptor shortens the duration of remifentanil-induced postoperative hyperalgesia by upregulating KCC2 in the spinal dorsal horn in rats. Mol Pain. 2017 Jan-Dec;13:1744806917704769. doi: 10.1177/1744806917704769. PubMed PMID: 28425312.

2: Silvestre de Ferron B, Vilpoux C, Kervern M, Robert A, Antol J, Naassila M, Pierrefiche O. Increase of KCC2 in hippocampal synaptic plasticity disturbances after perinatal ethanol exposure. Addict Biol. 2016 Oct 25. doi: 10.1111/adb.12465. [Epub ahead of print] PubMed PMID: 27778437.

3: Chevy Q, Heubl M, Goutierre M, Backer S, Moutkine I, Eugène E, Bloch-Gallego E, Lévi S, Poncer JC. KCC2 Gates Activity-Driven AMPA Receptor Traffic through Cofilin Phosphorylation. J Neurosci. 2015 Dec 2;35(48):15772-86. doi: 10.1523/JNEUROSCI.1735-15.2015. PubMed PMID: 26631461.

4: Uwera J, Nedergaard S, Andreasen M. A novel mechanism for the anticonvulsant effect of furosemide in rat hippocampus in vitro. Brain Res. 2015 Nov 2;1625:1-8. doi: 10.1016/j.brainres.2015.08.014. Epub 2015 Aug 21. PubMed PMID: 26301821.

5: Wang Y, Summers T, Peterson W, Miiller E, Burrell BD. Differential effects of GABA in modulating nociceptive vs. non-nociceptive synapses. Neuroscience. 2015 Jul 9;298:397-409. doi: 10.1016/j.neuroscience.2015.04.040. Epub 2015 Apr 27. PubMed PMID: 25931332.

6: Hamidi S, Avoli M. KCC2 function modulates in vitro ictogenesis. Neurobiol Dis. 2015 Jul;79:51-8. doi: 10.1016/j.nbd.2015.04.006. Epub 2015 Apr 26. PubMed PMID: 25926348; PubMed Central PMCID: PMC4880462.

7: Ford A, Castonguay A, Cottet M, Little JW, Chen Z, Symons-Liguori AM, Doyle T, Egan TM, Vanderah TW, De Konnick Y, Tosh DK, Jacobson KA, Salvemini D. Engagement of the GABA to KCC2 signaling pathway contributes to the analgesic effects of A3AR agonists in neuropathic pain. J Neurosci. 2015 Apr 15;35(15):6057-67. doi: 10.1523/JNEUROSCI.4495-14.2015. Erratum in: J Neurosci. 2015 Jun 10;35(23):8971. PubMed PMID: 25878279; PubMed Central PMCID: PMC4397603.

8: Hamidi S, D'Antuono M, Avoli M. On the contribution of KCC2 and carbonic anhydrase to two types of in vitro interictal discharge. Pflugers Arch. 2015 Nov;467(11):2325-35. doi: 10.1007/s00424-015-1686-4. Epub 2015 Jan 22. PubMed PMID: 25603963; PubMed Central PMCID: PMC4880467.

9: Deisz RA, Wierschke S, Schneider UC, Dehnicke C. Effects of VU0240551, a novel KCC2 antagonist, and DIDS on chloride homeostasis of neocortical neurons from rats and humans. Neuroscience. 2014 Sep 26;277:831-41. doi: 10.1016/j.neuroscience.2014.07.037. Epub 2014 Jul 30. PubMed PMID: 25086309.

10: Dzhala V, Valeeva G, Glykys J, Khazipov R, Staley K. Traumatic alterations in GABA signaling disrupt hippocampal network activity in the developing brain. J Neurosci. 2012 Mar 21;32(12):4017-31. doi: 10.1523/JNEUROSCI.5139-11.2012. PubMed PMID: 22442068; PubMed Central PMCID: PMC3333790.