Name: KRM-II-81
Brand: TargetMol
SKU: T27744
Rating: 4.5 (1 reviews)

规格

价格

库存

数量

25 mg

待询

8-10周

50 mg

待询

8-10周

100 mg

待询

8-10周

生物活性

产品描述	KRM-II-81 is an α2/α3-subtype-selective positive allosteric modulator of GABAA receptors. It potentiates GABA currents with an ED₅₀ of 32 nM in isolated dorsal root ganglion cultures and demonstrates anticonvulsant activity, including suppression of pharmaco-resistant seizures in amygdala-kindled rats (ED₅₀ = 19 mg/kg, i.p.) and reduction of hyperexcitability in traumatic brain injury models. Researchers utilize this compound to investigate the therapeutic potential of subtype-selective GABAergic modulation across pain-depressed behavior, neuropathic pain, and epilepsy assays, with a reduced motor impairment profile compared to non-selective benzodiazepines.
体内活性	KRM-II-81 是一种选择性作用于含α2/3亚基GABAA受体的正向别构调节剂。在动物模型中，小鼠腹腔注射可完全抑制6 Hz（44 mA）电刺激诱发的惊厥发作，且不改变转棒实验中的运动协调能力。口服给药（100 mg/kg）能显著延长戊四氮诱导的阵挛性和强直性惊厥潜伏期，并降低致死率。该化合物在啮齿类癫痫模型中展现出明确的抗惊厥效力，给药方式涵盖腹腔注射和口服灌胃，药效终点包括惊厥阈值、潜伏期及生存率等指标。
别名	KRM-II81, KRM-II 81

化学信息

分子量	351.36
分子式	C₂₁H₁₃N₅O
CAS No.	2014348-91-3
Smiles	C(#C)C=1C=C2C(N3C(=C(N=C3)C4=CN=CO4)CN=C2C5=CC=CC=N5)=CC1
密度	1.33 g/cm3 (Predicted)

储存&溶解度

存储	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. 实际储存温度请以COA为准

KRM-II-81