13585831301
021-59541103 021-60443211
3004967995
13585831301021-59541103 021-604432113004967995
在線訂購 免費訂購熱線：021-59541103 021-60443211
聯系人:高小姐
電話:021-59541103 021-60443211
手機:13585831301
Q Q： 3004967995
Email:3004967995@qq.com
詳細地址：上海嘉定區嘉羅公路1661
化學性質：
| 規格 | 1mg 5mg 10mg 25mg 50mg |
| CAS | 1173023-36-3 |
| 別名 | N/A |
| 化學名 | N/A |
| 分子式 | C18H20Cl2N4 |
| 分子量 | 363.28 |
| 溶解度 | DMSO: 62.5 mg/mL (172.04 mM) |
| 儲存條件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述：
L-745870 hydrochloride is a high-affinity, selective and orally active human dopamine D4 receptor antagonist with a Ki of 0.43 nM, and considerably weaker D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors affinity. L-745870 hydrochloride has excellent brain penetration[1][2][3].
In vitro pharmacological studies revealed that L-745870 is an antagonist at human D4 receptors, in that L-745870 is capable of antagonizing the ability of D4 receptors to inhibit agonist-induced stimulation of [35S]-GTPgS binding; blocking the inhibition of forskolin-stimulated adenylate cyclase activity in transfected human embryonic kidney (HEK293) and Chinese hamster ovary (CHO) cells; blocking dopamine-induced inhibition of Ca2+ currents in transfected GH4C1 pituitary cells; inhibiting D4 activation of cloned G protein-coupled inwardly rectifying K+ channels; and antagonizing dopamine-induced stimulation of extracellular acidification in transfected cells[1][2].
L-745870 has good pharmacokinetic properties (20-60% oral bioavailability and plasma t1/2 2.1-2.8 hours) in both rat and monkey, and excellent brain penetration with high brain to plasma ratios in rat[2].Evaluation of L-745870 in surrogate marker assays demonstrates that this compound is freely available for biological activity in the brain and that at doses of 5 to 60 mg/kg p.o. L-745870 would occupy 50% D4 receptors in the brain. L-745870 has no effect on apomorphine-induced stereotypy in rats but does induce catalepsy in mice, albeit at a high dose of 100 mg/kg p.o. that is likely to occupy D2 receptors in vivo. High doses of L-745870 might also be expected to cause extrapyramidal symptoms in primates because the levels in the CNS at these doses would be sufficient to antagonize D2 receptors. Following oral administration to squirrel monkeys, L745870 (10 mg/kg p.o.) induces mild sedation and extrapyramidal motor symptoms, notably bradykinesia, became apparent at 30 mg/kg. Lower doses of L-745870 has no observable behavioural effects in monkeys[1][2].
[1]. Bristow LJ, et al. Schizophrenia and L-745,870, a novel dopamine D4 receptor antagonist. Trends Pharmacol Sci. 1997 Jun;18(6):186-8. [2]. Patel S, et al. Biological profile of L-745,870, a selective antagonist with high affinity for the dopamine D4 receptor. J Pharmacol Exp Ther. 1997 Nov;283(2):636-47. [3]. Kulagowski JJ, et al. 3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor. J Med Chem. 1996 May 10;39(10):1941-2.
特別提醒：
1. 本產品僅供科研使用。請勿用于醫藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區。
2. 為了您的安全和健康，請穿好實驗服并佩戴一次性手套和口罩操作。
原創作者：上海莼試生物技術有限公司
留言注意事項：
1.遵守中華人民共和國有關法律、法規，尊重網上道德，承擔一切因您的行為而直接或間接引起的法律責任。
2.請您真實的反映產品的情況,不要捏造、誣蔑、造謠。如對產品有任何疑問,也可以留言咨詢。
3.未經本站同意，任何人不得利用本留言簿發布個人或團體的具有廣告性質的信息或類似言論。
| 您感興趣的產品* | |
| 您的單位* | |
| 聯系人* | |
| 聯系電話* | |
| 詳細地址* | |
| 常用郵箱* | |
| 請輸入您對我們的意見或建議* | |
| 驗證碼* | |
 |
產品訂購說明:
1、報價含普票、運費。
2、常用試劑備貨充足，除對溫度要求極其嚴格的產品當天可發貨。
3、進口原裝產品要3-6周的貨期，詳細情況請咨詢客服。
4、訂貨時間為工作日每周一至周五16:00之前。
5、如需代為檢測，標本對環境溫度高，可聯系客服安排專人取樣（限省內客戶）。
6、代測免收代測費，一周出結果。
7、產品因運輸途中包裝破損請拒絕簽收，做退回。我們將在24小時之內為您補發 損壞產品。
8、如因單位財務制度原因，可申請先發貨，報賬后付款（此條款僅限醫院、學校信譽良好客戶）。
普票匯款信息
賬 戶 名：上海生物
開 戶 行：中國銀行山東省分行營業部
賬 號：2169 2341 6278
關于莼試
產品訂購
新手指南
幫助中心