VU 0463271
- Product Name
- VU 0463271
- CAS No.
- 1391737-01-1
- Chemical Name
- VU 0463271
- Synonyms
- VU 0463271;VU0463271, 10 mM in DMSO;Inhibitor,KcsA,VU0463271,Potassium Channel,VU 0463271,VU-0463271,inhibit;N-Cyclopropyl-N-(4-methylthiazol-2-yl)-2-((6-phenylpyridazin-3-yl)thio)acetamide;N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide;Acetamide, N-cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]-;VU0463271 (N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide);VU0463271 (Synonyms: N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide)
- CBNumber
- CB74668658
- Molecular Formula
- C19H18N4OS2
- Formula Weight
- 382.5
- MOL File
- 1391737-01-1.mol
VU 0463271 Property
- storage temp.
- 2-8°C
- solubility
- Soluble in DMSO
- form
- powder
- color
- off-white to blue-gray
N-Bromosuccinimide Price
- Product number
- SML2333
- Product name
- VU0463271
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $89
- Updated
- 2025/07/31
- Product number
- SML2333
- Product name
- VU0463271
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $359
- Updated
- 2025/07/31
- Product number
- 4719
- Product name
- VU0463271
- Purity
- ≥98%(HPLC)
- Packaging
- 10
- Price
- $196
- Updated
- 2021/12/16
- Product number
- 4719
- Product name
- VU0463271
- Purity
- ≥98%(HPLC)
- Packaging
- 50
- Price
- $825
- Updated
- 2021/12/16
- Product number
- 257069
- Product name
- VU 0463271
- Packaging
- 10mg
- Price
- $432
- Updated
- 2021/12/16
VU 0463271 Chemical Properties,Usage,Production
Uses
VU 0463271 is a novel antagonist of the neuronal-specific potassium-chloride cotransporter 2 (KCC2).
Biological Activity
VU0463271 is a potent and selective potassium-chloride cotransporter 2 (KCC2) inhibitor th at displays greatly enhanced potency than its structural analogs VU0255011 (ML077) & VU0240511 (IC50 = 61, 537, and 568 nM, respectively). VU0463271 exhibits much reduced efficacy against the related Na-K-2Cl cotransporter 1 (NKCC1 inhibition max ~37% at 100 μM) and little affinity toward a panel of 68 GPCRs, ion channels, and transporters. Although VU0463271 is reported to exhibit affinity toward mitochondrial translocator protein TSPO (IC50 of 204 nM against PK11195 binding; r at heart) and inhibitory potency against α1B adrenergic receptor (IC50 of 364.7 nM; human α1B CHO transfectants), these proteins are not known to affect chloride homeostasis.
in vivo
VU0463271 is found to be a moderate-to-high clearance compound in rat (CL=57 mL/min/kg) following intravenous administration (1 mg/kg); the low volume of distribution at steady state (Vss 0.4 L/kg), coupled with moderate-to-high clearance produce a relatively short t1/2 (9 min) in vivo[1].
storage
Store at +4°C
VU 0463271 Preparation Products And Raw materials
Raw materials
Preparation Products
VU 0463271 Suppliers
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