CLP-290 | CAS#1181083-81-7 | KCC2 modulator

MedKoo Cat#: 527466 | Name: CLP-290

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Description:

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

CLP-290 is a novel KCC2 modulator and prodrug of CLP-257, highly selective for KCC2 over related Cl- transporters.

Chemical Structure

CLP-290

CAS#1181083-81-7

Theoretical Analysis

MedKoo Cat#: 527466

Name: CLP-290

CAS#: 1181083-81-7

Chemical Formula: C19H21FN4O3S

Exact Mass: 404.1318

Molecular Weight: 404.46

Elemental Analysis: C, 56.42; H, 5.23; F, 4.70; N, 13.85; O, 11.87; S, 7.93

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 350.00	2 Weeks
25mg	USD 650.00	2 Weeks

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Related CAS #

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Synonym

CLP290; CLP 290; CLP-290

IUPAC/Chemical Name

[5-Fluoro-2-[(Z)-(2-hexahydropyridazin-1-yl-4-oxo-thiazol-5-ylidene)methyl]phenyl] pyrrolidine-1-carboxylate

InChi Key

DIXMMXNNKLCLOM-WJDWOHSUSA-N

InChi Code

InChI=1S/C19H21FN4O3S/c20-14-6-5-13(15(12-14)27-19(26)23-8-3-4-9-23)11-16-17(25)22-18(28-16)24-10-2-1-7-21-24/h5-6,11-12,21H,1-4,7-10H2/b16-11-

SMILES Code

O=C(N1CCCC1)OC2=CC(F)=CC=C2/C=C(SC(N3CCCCN3)=N4)/C4=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

View handling instruction

Biological target:

CLP290 is an orally available activator of the neuron-specific K+-Cl− cotransporter KCC2.

In vitro activity:

TBD

In vivo activity:

Midazolam administration after pretreatment with CLP290 exerted inhibitory effects on neuronal activity exclusively in the somatosensory cortex of neonatal rats, which is consistent with the behavioral results in the righting reflex test shown in Fig 2. Reference: PLoS One. 2021; 16(3): e0248113. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7954344/

	Solvent	mg/mL	mM
Solubility
	DMSO	23.7	58.70
	DMSO:PBS (pH 7.2) (1:6)	1.0	2.47
	DMF	1.0	2.47
	Ethanol	2.0	4.99

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 404.46 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. Doi A, Miyazaki T, Mihara T, Ikeda M, Niikura R, Andoh T, Goto T. CLP290 promotes the sedative effects of midazolam in neonatal rats in a KCC2-dependent manner: A laboratory study in rats. PLoS One. 2021 Mar 12;16(3):e0248113. doi: 10.1371/journal.pone.0248113. PMID: 33711029; PMCID: PMC7954344.

In vitro protocol:

TBD

In vivo protocol:

1: Kim YB, Kim WB, Jung WW, Jin X, Kim YS, Kim B, Han HC, Block GD, Colwell CS, Kim YI. Excitatory GABAergic Action and Increased Vasopressin Synthesis in Hypothalamic Magnocellular Neurosecretory Cells Underlie the High Plasma Level of Vasopressin in Diabetic Rat. Diabetes. 2017 Dec 6. pii: db171042. doi: 10.2337/db17-1042. [Epub ahead of print] PubMed PMID: 29212780. 2: 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. PubMed PMID: 28634406; PubMed Central PMCID: PMC5478677.