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  2. Metabolic Enzyme/Protease Immunology/Inflammation GPCR/G Protein Neuronal Signaling
  3. MAGL Histamine Receptor
  4. JZP-361

JZP-361是一種有效的、可逆的、選擇性的人重組 MAGL (hMAGL) 抑制劑，IC50 為 46 nM。JZP-361 還具有抗組胺能活性，可用于哮喘的研究。

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JZP-361 Chemical Structure

JZP-361 Chemical Structure

CAS No. : 1680193-80-9

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3.  試用裝只面向終端客戶。

規(guī)格 價格 是否有貨 數(shù)量
1 mg ￥213
In-stock
5 mg ￥498
In-stock
10 mg ￥810
In-stock
25 mg ￥1475
In-stock
50 mg ￥2488
In-stock
100 mg ￥3388
In-stock
200 mg   詢價  
500 mg   詢價  

* Please select Quantity before adding items.

Customer Review

查看 Histamine Receptor 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

JZP-361 is a potent, reversible and selective inhibitor of human recombinant MAGL (hMAGL) with an IC50 of 46 nM. JZP-361 also shows antihistaminergic activities and can be used for asthma research[1].

IC50 & Target

hMAGL

46 nM (IC50)

hABHD6

1.79 μM (IC50)

hFAAH

7.24 μM (IC50)

H1 Receptor

6.81 (pA2)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
COS-7 IC50
7.24 μM
Compound: JZP-361
Inhibition of human FAAH expressed in COS7 cell membranes pre-incubated for 10 mins before [3H]-AEA substrate addition by liquid scintillation counting
Inhibition of human FAAH expressed in COS7 cell membranes pre-incubated for 10 mins before [3H]-AEA substrate addition by liquid scintillation counting
[PMID: 26344596]
HEK293 IC50
0.046 μM
Compound: JZP-361
Inhibition of human MAGL expressed in HEK293 cells pre-incubated for 10 mins before 2-AG substrate addition by HPLC method
Inhibition of human MAGL expressed in HEK293 cells pre-incubated for 10 mins before 2-AG substrate addition by HPLC method
[PMID: 26344596]
HEK293 IC50
1.78 μM
Compound: JZP-361
Inhibition of human ABHD6 expressed in HEK293 cells assessed as reduction in glycerol production from 1-AG hydrolysis pre-incubated for 30 mins before 1-AG substrate addition and measured 90 mins post substrate addition by fluorescence method
Inhibition of human ABHD6 expressed in HEK293 cells assessed as reduction in glycerol production from 1-AG hydrolysis pre-incubated for 30 mins before 1-AG substrate addition and measured 90 mins post substrate addition by fluorescence method
[PMID: 26344596]
體外研究
(In Vitro)

JZP-361 has almost 150-fold higher selectivity over human recombinant fatty acid amide hydrolase (hFAAH, IC50 = 7.24 μM) and 35-fold higher selectivity over human α/β-hydrolase-6 (hABHD6, IC50 = 1.79 μM)[1].
JZP-361 retains H1 antagonistic affinity (pA2 = 6.81) but did not show cannabinoid receptor activity, when tested at concentrations ≤10 μM[1].
JZP-361 displays favorable interactions within the active site of hMAGL including the important hydrogen-bonding of the carbonyl oxygen to the oxyanion hole[1].

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

405.88

Formula

C22H20ClN5O
CAS 號
性狀

固體

顏色

White to off-white

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
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)
細(xì)胞實驗： 

DMSO 中的溶解度 : 125 mg/mL (307.97 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.4638 mL 12.3189 mL 24.6378 mL
5 mM 0.4928 mL 2.4638 mL 4.9276 mL
查看完整儲備液配制表

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

  • 摩爾計算器

  • 稀釋計算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻(xiàn)

完整儲備液配制表

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

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4638 mL 12.3189 mL 24.6378 mL 61.5946 mL
5 mM 0.4928 mL 2.4638 mL 4.9276 mL 12.3189 mL
10 mM 0.2464 mL 1.2319 mL 2.4638 mL 6.1595 mL
15 mM 0.1643 mL 0.8213 mL 1.6425 mL 4.1063 mL
20 mM 0.1232 mL 0.6159 mL 1.2319 mL 3.0797 mL
25 mM 0.0986 mL 0.4928 mL 0.9855 mL 2.4638 mL
30 mM 0.0821 mL 0.4106 mL 0.8213 mL 2.0532 mL
40 mM 0.0616 mL 0.3080 mL 0.6159 mL 1.5399 mL
50 mM 0.0493 mL 0.2464 mL 0.4928 mL 1.2319 mL
60 mM 0.0411 mL 0.2053 mL 0.4106 mL 1.0266 mL
80 mM 0.0308 mL 0.1540 mL 0.3080 mL 0.7699 mL
100 mM 0.0246 mL 0.1232 mL 0.2464 mL 0.6159 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

產(chǎn)品名稱：
JZP-361
目錄號：
HY-121422
需求量：