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61350-00-3

中文名稱 VU 0364770
英文名稱 VU 0364770
CAS 61350-00-3
分子式 C12H9ClN2O
分子量 232.67
MOL 文件 61350-00-3.mol
更新日期 2024/12/24 22:20:10
61350-00-3 結(jié)構(gòu)式 61350-00-3 結(jié)構(gòu)式

基本信息

中文別名
N-(3-氯苯基)吡啶甲酰胺
N-(3-氯苯基)-2-吡啶甲酰胺
英文別名
VU 0364770
VU 0364770 100MG
VU 0364770 USP/EP/BP
VU0364770
VU-0364770
N-(3-Chlorophenyl)picolinamide
N-(3-chlorophenyl)pyridine-2-carboxamide
2-PyridinecarboxaMide, N-(3-chlorophenyl)-
所屬類別
生物化工:GluR 拮抗劑

物理化學(xué)性質(zhì)

熔點(diǎn)81-83 °C
沸點(diǎn)293.6±20.0 °C(Predicted)
密度1.341±0.06 g/cm3(Predicted)
儲(chǔ)存條件Inert atmosphere,Store in freezer, under -20°C
溶解度DMF: 30 mg/ml; DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml; DMSO: 25 mg/ml; Ethanol: 5 mg/ml
酸度系數(shù)(pKa)11.24±0.70(Predicted)
形態(tài)粉末
顏色Light yellow to yellow

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335

應(yīng)用領(lǐng)域

用途1
N-(3-Chlorophenyl)-2-pyridinecarboxamide shows positive allosteric modulation at the mGlu4 receptors in combination with other antagonists resulting in treatment for the neurodegenerative Parkinson鈥檚 disease.
VU 0364770價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2024/11/08HY-100588VU 0364770
VU0364770
61350-00-35mg350元
2024/11/08HY-100588VU 0364770
VU0364770
61350-00-310mg520元
2024/11/08HY-100588VU 0364770
VU0364770
61350-00-325mg900元

常見問題列表

生物活性
VU0364770 是一種有效的選擇性 mGlu4 正變構(gòu)調(diào)節(jié)劑 (PAM)。VU0346770 對(duì)大鼠 mGlu4 和人 mGlu4 受體的 EC50 分別為 290 nM 和 1.1 μM。VU0364770 對(duì) mGlu5 具有拮抗活性,EC50 為 17.9 μM,VU0364770 對(duì) mGlu6 具有正變構(gòu)調(diào)節(jié)活性,EC50 為 6.8 μM。VU0364770 還對(duì) MAO 具有活性,作用于人 MAO-A 和 MAO-B 的 Ki 值分別為8.5 和 0.72 μM。
靶點(diǎn)

Rat mGlu 4

290 nM (EC 50 )

Human mGlu 4

1.1 μM (EC 50 )

mGlu 6

6.8 μM (EC 50 )

mGlu 5

17.9 μM (EC 50 )

體外研究

VU0364770 is a selective positive allosteric modulator of mGlu 4 in recombinant systems. VU0364770 is a potent PAM of multiple signaling pathways that enhances the response of the rat and human mGlu 4 receptors to the endogenous agonist glutamate. VU0364770 produces a concentration-dependent potentiation of the response to an EC 20 concentration of glutamate with EC 50 of 1.1±0.2 μM and increases the maximal response to glutamate from 100 to 227±17%. Because of concerns that this chemical scaffold might possess activity at MAO, full IC 50 determinations is performed for VU0364770 at the MAO-A and MAO-B isoforms; these studies result in K i s of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively. When tested at a 10 μM concentration at each mGlu receptor, VU0364770 exhibits weak PAM activity (4.3-fold left shift of the glutamate CRC) at mGlu6 and antagonist activity (3.3-fold right shift of the glutamate CRC) at mGlu5 (compare to the 16.5-fold left shift of the glutamate concentration-response for mGlu 4 at 10 μM). When further evaluated in a full concentration-response curve format, VU0364770 exhibits antagonist activity at mGlu 5 with a potency of 17.9±5.5 μM and PAM activity at mGlu 6 with a potency of 6.8±1.7 μM (compare with the potency of VU0364770 on the rat mGlu 4 receptor of 290±80 nM).

體內(nèi)研究

VU0364770 exhibits suitable pharmacokinetic properties for systemic dosing in animal models. After intravenous administration, VU0364770 is rapidly clears from the systemic circulation (165 ml/min/kg) and exhibits a volume of distribution of 2.92 L/kg. VU0364770 is a highly protein-bound ligand displaying free fractions of 2.7 and 1.8% in human and rat plasma, respectively. VU0364770 also shows an improved pharmacokinetic profile relative to previously reported mGlu 4 PAMs with enhanced central penetration and a total brain-to-plasma ratio of more than 1 after systemic administration of a 10 mg/kg dose. VU0364770 produces a dose-dependent reversal of haloperidol-induced catalepsy. VU0364770 dose-dependently reverses haloperidol (0.75 mg/kg)-induced catalepsy in rats, significant at doses of 10 to 56.6 mg/kg, after subcutaneous dosing (F 6,69 =8.04; p<0.001).

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