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  2. GPCR/G Protein Neuronal Signaling
  3. Cannabinoid Receptor
  4. SR144528

SR144528 是一個(gè)有效且選擇性的 CB2 受體拮抗劑，其 Ki 值為 0.6 nM。

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SR144528 Chemical Structure

SR144528 Chemical Structure

CAS No. : 192703-06-3

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1089
In-stock
1 mg ￥396
In-stock
5 mg ￥990
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10 mg ￥1750
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25 mg ￥3900
In-stock
50 mg 現(xiàn)貨 詢價(jià)
100 mg   詢價(jià)  
200 mg   詢價(jià)  

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查看 Cannabinoid Receptor 亞型特異性產(chǎn)品:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

SR144528 is a potent and selective CB2 receptor antagonist with a Ki of 0.6 nM.

IC50 & Target

CB2

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO-K1 EC50
26.69 μM
Compound: SR144528
Inverse agonist activity at recombinant human CB2R expressed in CHOK1 cells assessed as increase in NKH477-stimulated intracellular cAMP levels after 30 mins by chemiluminescent based cAMP Hunter assay
Inverse agonist activity at recombinant human CB2R expressed in CHOK1 cells assessed as increase in NKH477-stimulated intracellular cAMP levels after 30 mins by chemiluminescent based cAMP Hunter assay
[PMID: 32515588]
HEK293 EC50
23.31 nM
Compound: 1, SR144528
Antagonist activity at CB2 receptor in HEK293 cells assessed as increase in CP-55,940 EC50 measuring inhibition of forskolin-stimulated cAMP accumulation at 1 uM incubated 20 mins prior to CP-55,940 addition measured after 7 mins by spectrophotometry (Rvb
Antagonist activity at CB2 receptor in HEK293 cells assessed as increase in CP-55,940 EC50 measuring inhibition of forskolin-stimulated cAMP accumulation at 1 uM incubated 20 mins prior to CP-55,940 addition measured after 7 mins by spectrophotometry (Rvb
[PMID: 23855811]
HEK293 IC50
541.9 μM
Compound: SR144528
Displacement of 3[H]-CP55940 from human recombinant CB1 receptor expressed in HEK293 cell membranes measured after 90 mins
Displacement of 3[H]-CP55940 from human recombinant CB1 receptor expressed in HEK293 cell membranes measured after 90 mins
[PMID: 31185414]
HEK293 IC50
7.16 μM
Compound: SR144528
Displacement of 3[H]-CP55940 from human recombinant CB2 receptor expressed in HEK293 cell membranes measured after 90 mins
Displacement of 3[H]-CP55940 from human recombinant CB2 receptor expressed in HEK293 cell membranes measured after 90 mins
[PMID: 31185414]
HEK293 IC50
96.2 nM
Compound: SR144528
Inverse agonist activity at human CB2 receptor expressed in HEK293 EBNA cell membranes after 30 mins by [35S]-GTPgammaS binding assay
Inverse agonist activity at human CB2 receptor expressed in HEK293 EBNA cell membranes after 30 mins by [35S]-GTPgammaS binding assay
[PMID: 28088085]
體外研究
(In Vitro)

SR144528 是一種有效的選擇性 CB2 受體拮抗劑，Ki 為 0.6 nM。SR144528 單獨(dú)能夠以濃度依賴性方式 (EC50=26±6 nM，兩個(gè)實(shí)驗(yàn)) 刺激 CHO-CB2 細(xì)胞中毛喉素敏感的腺苷酸環(huán)化酶活性，在 1 μM 時(shí)效果最大 (4 倍刺激) 而在此濃度下，它對(duì) CHO-CB1 細(xì)胞沒(méi)有顯著影響 (15% 抑制)[1]。輔以 SR144528 的原始 264.7 巨噬細(xì)胞顯示降低的 caspase-3 活性。SR144528 以濃度依賴性方式抑制微粒體酰基輔酶 A：膽固醇?；D(zhuǎn)移酶 (ACAT) 活性，IC50 值為 3.6±1.1 μM。在 10 μM 時(shí)，SR144528 抑制約 68% 的 ACAT 活性[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

SR144528 在口服 (10 mg/kg) 或 icv (10 μg/動(dòng)物) 給藥后，未觀察到 [3H]-CP 55,940 與小鼠大腦特定位點(diǎn)的結(jié)合 。SR144528 對(duì)脾臟大麻素受體的占據(jù)具有時(shí)間依賴性，并且在口服給藥 3 mg/kg 后至少 18 h 內(nèi)顯著[1]。
SR144528 單獨(dú)給藥時(shí)不會(huì)對(duì)胃腸 (GI) 運(yùn)動(dòng)產(chǎn)生任何顯著影響。SR144528 不會(huì)阻斷但會(huì)增強(qiáng)胃排空延遲[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

476.05

Formula

C29H34ClN3O
CAS 號(hào)
性狀

固體

顏色

White to light yellow

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 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)：