Darapladib (SB-480848) 返回列表頁(yè)

參考價(jià):1300

具體成交價(jià)以合同協(xié)議為準(zhǔn)

型號(hào)
HY-10521
品牌
MCE
廠(chǎng)商性質(zhì)
代理商
所在地
杭州市

規(guī)格

5mg 1300元 10000支可售

在線(xiàn)詢(xún)價(jià) 加入對(duì)比查看聯(lián)系電話(huà)

聯(lián)系方式：鄧女士查看聯(lián)系方式

更新時(shí)間：2024-06-24 17:34:23瀏覽次數(shù)：267次

聯(lián)系我時(shí)，請(qǐng)告知來(lái)自制藥網(wǎng)

CAS號(hào)	356057-34-6	產(chǎn)地	國(guó)產(chǎn)
規(guī)格	5mg	級(jí)別	化工級(jí)
證書(shū)	ISO系列證書(shū)

CAS號(hào)

356057-34-6

產(chǎn)地

國(guó)產(chǎn)

規(guī)格

5mg

級(jí)別

化工級(jí)

證書(shū)

ISO系列證書(shū)

Darapladib (Synonyms: SB-480848)

Darapladib 是一種有效的脂蛋白相關(guān)磷脂酶A2抑制劑，IC₅₀ 為 0.25 nM。

生物活性

Darapladib is a potent inhibitor of lipoprotein-associated phospholipase A2with IC₅₀ of 0.25 nM.

IC₅₀ & Target

IC50: 0.25 nM (Lp-PLA₂)^[1]

體外研究(In Vitro)

Mechanistic studies using steady state and transient kinetics indicate Darapladib (SB-480848) to be a freely reversible, non-covalently bound, inhibitor of rhLp-PLA₂ with a K_i of 110 pM and an off-rate of 27 min. Potent inhibition of the enzyme in whole human plasma is confirmed (IC₅₀=5±2 nM). Furthermore, the presence of Darapladib during the copper catalysed oxidation of human LDL prevents the production of lyso-PtdCho (IC₅₀=4±3 nM) and subsequent monocyte chemotaxis (IC₅₀=4±1 nM)^[1].

體內(nèi)研究(In Vivo)

Additional in vivo studies with Darapladib indicated an oral bioavailability of 11±2% in the fed rat. The oral bioavailability of Darapladib is 28±4% in the dog. Furthermore excellent inhibition of Lp-PLA₂ within the atherosclerotic plaque is achieved for Darapladib, with 95±1% inhibition observed 2 h after an oral dose of 30 mg/kg to the WHHL rabbit^[1]. Darapladib, a specific inhibitor of lipoprotein-associated phospholipase A2 (lp-PLA₂), on inflammation and atherosclerotic formation in the low density lipoprotein receptor (LDLR)-deficient mice. the activity of serum lp-PLA₂ is inhibited by more than 60% in LDLR-deficient mice after oral administration of 50 mg/kg once daily of Darapladib for 6 weeks. Darapladib significantly inhibits serum lp-PLA₂ activity in LDLR-deficient mice^[2].

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01711723	GlaxoSmithKline	Atherosclerosis	October 29, 2012	Phase 1
NCT01873339	GlaxoSmithKline	Atherosclerosis	June 19, 2013	Phase 1
NCT01154114	GlaxoSmithKline	Atherosclerosis	July 1, 2010	Phase 1

分子量：666.77

性狀：Solid

Formula：C₃₆H₃₈F₄N₄O₂S

CAS 號(hào)：356057-34-6

中文名稱(chēng)：達(dá)拉地；達(dá)普拉締

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性數(shù)據(jù)

In Vitro:

DMSO : ≥ 100 mg/mL (149.98 mM)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	1.4998 mL	7.4988 mL	14.9977 mL
5 mM	0.3000 mL	1.4998 mL	2.9995 mL
10 mM	0.1500 mL	0.7499 mL	1.4998 mL

請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。

In Vivo:

請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥方式選擇適當(dāng)?shù)娜芙夥桨浮Ｒ韵氯芙夥桨付颊?qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：

——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

1.

請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (3.75 mM); Clear solution
2.

請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (3.75 mM); Clear solution
3.

請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (3.75 mM); Clear solution

參考文獻(xiàn)

[1]. Blackie JA, et al. The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2. Bioorg Med Chem Lett. 2003 Mar 24;13(6):1067-70. [Content Brief]
[2]. Hu MM, et al. The inhibition of lipoprotein-associated phospholipase A2 exerts beneficial effects against atherosclerosis inLDLR-deficient mice. Acta Pharmacol Sin. 2011 Oct;32(10):1253-1258. [Content Brief]

注：產(chǎn)品僅用于科研