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(R)-(+)-HA-966

NMDA受体拮抗剂/部分激动剂,R)-(+)-HA-966 ((+)-HA-966) 是 N-甲基-D-天冬氨酸 (NMDA) 受体复合物的甘氨酸位点的部分激动剂/拮抗剂。

目录号: PC12097 纯度: ≥98%

CAS No. :123931-04-4

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中文名称

(R)-(+)-HA-966

中文别名

R(+)-3-氨基-1-羟基-2-吡咯烷酮;烯丙基(环戊基)镍;(3R)-3-氨基-1-羟基-2-吡咯烷酮

英文名称

(R)-(+)-HA-966

英文别名

2-Pyrrolidinone,3-amino-1-hydroxy-, (3R)-;(R)-(+)-HA-966;(R)-(+)-HA-966,(R)-(+)-3-Amino-1-hydroxypyrrolidin-2-one;R(+)-3-Amino-1-hydroxy-2-pyrrolidinone;(+)-HA 966;(R)-(+)-HA 966;(R)-HA 966;R(+)-HA-966 R(+)-3-AMINO-1-HYDROX;(3R)-3-Amino-1-hydroxy-2-pyrrolidinone;(R)-(+)-3-AMINO-1-HYDROXYPYRROLIDIN-2-ONE;(R)-3-amino-1-hydroxypyrrolidin-2-one 2,2,2-trifluoroacetate;Zinc03791818

Cas No.

123931-04-4

分子式

C₄H₉N₂O₂+

分子量

117.13

包装储存

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

(R)-(+)-HA-966 ((+)-HA-966) is a partial agonist/antagonist of glycine site of the N-methyl-D-aspartate (NMDA) receptor complex. (R)-(+)-HA-966 selectively blocks the activation of the mesolimbic dopamine system by amphetamine. (R)-(+)-HA-966 can cross the blood-brain barrier and has the potential for neuropathic and acute pain.

性状

Solid

IC50 & Target[1][2]

glycine site of the NMDA receptor

体内研究(In Vivo)

(R)-(+)-HA-966 ((+)-HA-966; 10 mg/kg; IV) significantly attenuates the dose-dependent pressor response and the associated tachycardic response elicited by systemic NMDA (125, 250, 500, and 1000 mg/kg; i.v.).
(+)-HA-966 (30, 100 mg/kg; IP) dose-dependently blocks the enhancement of dopamine synthesis induced in the nucleus accumbens by amphetamine, but is without effect on the increase in dopamine synthesis in the striatum in male BKTO mice (20-30g).

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Sprague-Dawley rats (11 to 12 weeks old)
Dosage:	10 mg/kg
Administration:	IV
Result:	Significantly attenuated the dose-dependent pressor response and the associated tachycardic response elicited by systemic NMDA.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Hutson PH, et al. R-(+)-HA-966, a glycine/NMDA receptor antagonist, selectively blocks the activation of the mesolimbic dopamine system by amphetamine. Br J Pharmacol. 1991 Aug;103(4):2037-44. [Information]

[2]. Witkin JM, et al. Discriminative stimulus effects of R-(+)-3-amino-1-hydroxypyrrolid-2-one, [(+)-HA-966], a partial agonist of the strychnine-insensitive modulatory site of the N-methyl-D-aspartate receptor. J Pharmacol Exp Ther. 1995 Dec;275(3):1267-73. [Information]

[3]. Christensen D, et al. The antinociceptive effect of combined systemic administration of morphine and the glycine/NMDA receptor antagonist, (+)-HA966 in a rat model of peripheral neuropathy. Br J Pharmacol. 1998 Dec;125(8):1641-50. [Information]

溶解度数据

体外研究:

H₂O : 125 mg/mL (1076.47 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	8.6118 mL	43.0589 mL	86.1178 mL
5 mM	1.7224 mL	8.6118 mL	17.2236 mL
10 mM	0.8612 mL	4.3059 mL	8.6118 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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