2. GPCR/G Protein
  3. LPL Receptor
  4. AMG 369

AMG 369 是一种口服有效的强效双重 S1P1/S1P5 激动剂，对 S1P3 的活性有限，对 S1P2/S1P4 无活性。AMG 369 可降低血液淋巴细胞计数。AMG 369 可延迟大鼠实验性自身免疫性脑脊髓炎的发病并降低其严重程度。

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AMG 369

AMG 369 Chemical Structure

CAS No. : 1202073-26-4

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AMG 369 相关抗体

Top Publications Citing Use of Products

查看 LPL Receptor 亚型特异性产品:

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LPAR1 LPAR2 LPAR3 LPAR5 S1PR1 S1PR2 S1PR3 S1PR4 S1PR5

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AMG 369 is an orally active and potent dual S1P1/S1P5 agonist with limited activity at S1P3 and no activity at S1P2/S1P4. AMG 369 reduces blood lymphocyte counts. AMG 369 delays onset and reduces severity of experimental autoimmune encephalomyelitis in rat[1].

IC50 & Target[1]

S1PR1

 

S1PR5

 

S1PR3

 

体外研究
(In Vitro)

AMG 369 可强效诱导 U2OS 细胞中 hS1P1-GFP 融合蛋白的内吞，其 EC50 为 0.002 μM，效能达 98%[1]。
AMG 369 可通过转染的 CHO-K1 细胞中的 hS1P3 微弱诱导 Ca2+ 动员，其 EC50 为 0.888 μM，效能为 26%[1]。

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

AMG 369 相关抗体:
体内研究
(In Vivo)

AMG 369 (0.01-0.1 mg/kg；口服；单次给药) 予雌性 Lewis 大鼠后，在给药后 24 小时，0.03 mg/kg 剂量下可使血液淋巴细胞计数显著降低 45%，0.1 mg/kg 剂量下可降低 65%，呈现剂量依赖性的统计学显著效应[1]。
AMG 369 (0.1 mg/kg；口服；单次给药) 可延缓雌性 Lewis 大鼠实验性自身免疫性脑脊髓炎模型的发病并降低临床疾病严重程度[1]。

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

Animal Model: Lewis rats (female)[1]
Dosage: 0.01 mg/kg; 0.03 mg/kg; 0.1 mg/kg
Administration: p.o.; single dose
Result: Produced a non-statistically significant reduction in blood lymphocytes at 0.01 mg/kg vs vehicle.
Produced a statistically significant 45% reduction in blood lymphocytes at 0.03 mg/kg vs vehicle.
Produced a statistically significant 65% reduction in blood lymphocytes at 0.1 mg/kg vs vehicle, nearly the maximal 70% reduction typically observed with S1P1 agonists.
Animal Model: Lewis rats (female; experimental autoimmune encephalomyelitis model induced by guinea pig myelin basic protein immunization)[1]
Dosage: 0.01 mg/kg; 0.1 mg/kg
Administration: p.o.; single dose
Result: Did not significantly impact clinical disease scores at 0.01 mg/kg vs vehicle.
Delayed disease onset and produced a statistically significant reduction in clinical disease scores at 0.1 mg/kg vs vehicle.
分子量

459.54

Formula

C26H22FN3O2S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

AMG 369 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

AMG 3691202073-26-4AMG369AMG-369LPL ReceptorLysophospholipid ReceptorS1P2multiple sclerosisS1P5S1P4U2OS cellsratS1P1lymphocytesexperimental autoimmune encephalomyelitisS1P3Inhibitorinhibitorinhibit

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产品名称：
AMG 369
目录号：
HY-14402
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