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MedKoo Cat#: 527683 | Name: CLP257
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Description:

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

CLP257 is a putative KCC2 upregulator. CLP257 improved chloride homeostasis and reduced the duration and frequency of ILDs in a concentration-dependent manner. CLP257 exhibits selectivity for KCC2 over other KCC family members. CLP257 enhances Cl- transport and increases KCC2 plasma membrane expression in spinal slices with reduced KCC2 function.

Chemical Structure

CLP257
CLP257
CAS#1181081-71-9

Theoretical Analysis

MedKoo Cat#: 527683

Name: CLP257

CAS#: 1181081-71-9

Chemical Formula: C14H14FN3O2S

Exact Mass: 307.0791

Molecular Weight: 307.34

Elemental Analysis: C, 54.71; H, 4.59; F, 6.18; N, 13.67; O, 10.41; S, 10.43

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 3,750.00 2 Weeks
2g USD 6,250.00 2 Weeks
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Related CAS #
No Data
Synonym
CLP 257; CLP-257; CLP257
IUPAC/Chemical Name
(5Z)-5-[(4-Fluoro-2-hydroxyphenyl)methylene]-2-(tetrahydro-1-(2H)-pyridazinyl)-4(5H)-thiazolone
InChi Key
SKCADXVKQRCWTR-GHXNOFRVSA-N
InChi Code
InChI=1S/C14H14FN3O2S/c15-10-4-3-9(11(19)8-10)7-12-13(20)17-14(21-12)18-6-2-1-5-16-18/h3-4,7-8,16,19H,1-2,5-6H2/b12-7-
SMILES Code
O=C1N=C(N2CCCCN2)S/C1=C\C3=CC=C(F)C=C3O
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

Preparing Stock Solutions

The following data is based on the product molecular weight 307.34 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
1: Gao Y, Zhan W, Jin Y, Chen X, Cai J, Zhou X, Huang X, Zhao Q, Wang W, Sun J. KCC2 receptor upregulation potentiates antinociceptive effect of GABAAR agonist on remifentanil-induced hyperalgesia. Mol Pain. 2022 Jan- Dec;18:17448069221082880. doi: 10.1177/17448069221082880. PMID: 35352582; PMCID: PMC8972932. 2: Paige C, Plasencia-Fernandez I, Kume M, Papalampropoulou-Tsiridou M, Lorenzo LE, David ET, He L, Mejia GL, Driskill C, Ferrini F, Feldhaus AL, Garcia- Martinez LF, Akopian AN, De Koninck Y, Dussor G, Price TJ. A Female-Specific Role for Calcitonin Gene-Related Peptide (CGRP) in Rodent Pain Models. J Neurosci. 2022 Mar 9;42(10):1930-1944. doi: 10.1523/JNEUROSCI.1137-21.2022. Epub 2022 Jan 20. PMID: 35058371; PMCID: PMC8916765. 3: Bilchak JN, Yeakle K, Caron G, Malloy D, Côté MP. Enhancing KCC2 activity decreases hyperreflexia and spasticity after chronic spinal cord injury. Exp Neurol. 2021 Apr;338:113605. doi: 10.1016/j.expneurol.2021.113605. Epub 2021 Jan 13. PMID: 33453210; PMCID: PMC7904648. 4: Dzhala VI, Staley KJ. KCC2 Chloride Transport Contributes to the Termination of Ictal Epileptiform Activity. eNeuro. 2021 Mar 9;8(2):ENEURO.0208-20.2020. doi: 10.1523/ENEURO.0208-20.2020. PMID: 33239270; PMCID: PMC7986536. 5: Jin X, Kim WB, Kim MN, Jung WW, Kang HK, Hong EH, Kim YS, Shim WJ, Han HC, Colwell CS, Kim YB, Kim YI. Oestrogen inhibits salt-dependent hypertension by suppressing GABAergic excitation in magnocellular AVP neurons. Cardiovasc Res. 2021 Aug 29;117(10):2263-2274. doi: 10.1093/cvr/cvaa271. PMID: 32960965. 6: Lizhnyak PN, Muldoon PP, Pilaka PP, Povlishock JT, Ottens AK. Traumatic Brain Injury Temporal Proteome Guides KCC2-Targeted Therapy. J Neurotrauma. 2019 Nov 15;36(22):3092-3102. doi: 10.1089/neu.2019.6415. Epub 2019 Jul 31. PMID: 31122143; PMCID: PMC6818491. 7: Gagnon M, Bergeron MJ, Perez-Sanchez J, Plasencia-Fernández I, Lorenzo LE, Godin AG, Castonguay A, Bonin RP, De Koninck Y. Reply to The small molecule CLP257 does not modify activity of the K+-Cl- co- transporter KCC2 but does potentiate GABAA receptor activity. Nat Med. 2017 Dec 7;23(12):1396-1398. doi: 10.1038/nm.4449. PMID: 29216044. 8: Cardarelli RA, Jones K, Pisella LI, Wobst HJ, McWilliams LJ, Sharpe PM, Burnham MP, Baker DJ, Chudotvorova I, Guyot J, Silayeva L, Morrow DH, Dekker N, Zicha S, Davies PA, Holenz J, Duggan ME, Dunlop J, Mather RJ, Wang Q, Medina I, Brandon NJ, Deeb TZ, Moss SJ. The small molecule CLP257 does not modify activity of the K+-Cl- co-transporter KCC2 but does potentiate GABAA receptor activity. Nat Med. 2017 Dec 7;23(12):1394-1396. doi: 10.1038/nm.4442. PMID: 29216042; PMCID: PMC7371006. 9: Ferrini F, Lorenzo LE, Godin AG, Quang ML, De Koninck Y. Enhancing KCC2 function counteracts morphine-induced hyperalgesia. Sci Rep. 2017 Jun 20;7(1):3870. doi: 10.1038/s41598-017-04209-3. PMID: 28634406; PMCID: PMC5478677. 10: 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. PMID: 25926348; PMCID: PMC4880462. 11: Bergeron MJ, Castonguay A, De Koninck Y. KCC2 : nouvelle cible thérapeutique pour le traitement de pathologies neurologiques [KCC2: a new therapeutical target for the treatment of neurological diseases]. Med Sci (Paris). 2014 May;30(5):514-7. French. doi: 10.1051/medsci/20143005013. Epub 2014 Jun 13. PMID: 24939537. 12: Gagnon M, Bergeron MJ, Lavertu G, Castonguay A, Tripathy S, Bonin RP, Perez- Sanchez J, Boudreau D, Wang B, Dumas L, Valade I, Bachand K, Jacob-Wagner M, Tardif C, Kianicka I, Isenring P, Attardo G, Coull JA, De Koninck Y. Chloride extrusion enhancers as novel therapeutics for neurological diseases. Nat Med. 2013 Nov;19(11):1524-8. doi: 10.1038/nm.3356. Epub 2013 Oct 6. PMID: 24097188; PMCID: PMC4005788.