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NS309

SKU: orb1222579

Description

NS309 is a nonselective activator of small- and intermediate-conductance Ca2+-activated K+ (SK/KCa2 and IK/KCa3.1) channels (EC50s range from 0.12-1.2 μM for SK channels and 10-90 nM for IK channels). It can also activate voltage-gated Kv11.1 channels (hERG; IC50 = 1 μM), but does not, however, affect large conductance (BK/KCa1.1) channels. NS309 can modulate neuronal firing patterns by enhancing SK-mediated hyperpolarizing effects. It is 730-fold (SK channels) and 7,400-fold (IK channels) more potent than 1-EBIO and often used in conjunction with CyPPA to distinguish between SK1 and SK3 subtypes.

Images & Validation

Key Properties

CAS Number18711-16-5
MW231.04
Purity>98% (HPLC)
FormulaC8H4Cl2N2O2
SMILESClc2ccc1c(NC(=O)C1=NO)c2Cl
TargetROS
SolubilityDMSO : ≥ 50 mg/mL; 216.41 mM

Bioactivity

In Vivo
NS309 (2 mg/kg; i.p.) protects against SCI/R in rabbits. Animal model: Adult New Zealand white rabbits (2.5-3.0 kg). Dosage: 2 mg/kg. Administration: Intraperitoneal injection. Result: Significantly improved neurological outcome of SCI/R challenged rabbits.
In Vitro
NS309 (40 nM) activates both hSK3 and hIK channels, with the largest effect on hIK channels (8.5-fold increase in current compares to 1.9-fold increase in current for hSK3 channels). NS309 (10 μM) significantly increases the whole cell SK currents and hyperpolarized detrusor smooth muscle (DSM) cells resting membrane potential. NS309 inhibits the spontaneous phasic contraction amplitude, force, frequency, duration and tone of isolated DSM strips in a concentration-dependent manner.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

NS309 | NS-309 | NS 309

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Protocol Information

NS309 (orb1222579)

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% DMSO +
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% Tween 80 +
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Available Sizes

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5 mg
$ 100.00
10 mg
$ 110.00
25 mg
$ 190.00
50 mg
$ 320.00
100 mg
$ 470.00
200 mg
$ 660.00
500 mg
$ 1,040.00