2. GPCR/G Protein
  3. LPL Receptor
  4. S1P1 agonist 5

S1P1 agonist 5 是一种选择性和具有口服活性的 S1P1 激动剂。S1P1 agonist 5 抑制淋巴细胞从淋巴组织排出到外周血。S1P1 agonist 5 具有研究多发性硬化症 (MS) 的潜力。

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S1P1 agonist 5 Chemical Structure

S1P1 agonist 5 Chemical Structure

CAS No. : 2760666-20-2

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S1P1 agonist 5 相关抗体

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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

S1P1 agonist 5 is a selective and orally active S1P1 agonist. S1P1 agonist 5 inhibits the lymphocyte egress from the lymphoid tissue to the peripheral blood. S1P1 agonist 5 has the potential for the research of multiple sclerosis (MS)[1].

体外研究
(In Vitro)

S1P1 agonist 5 (compound 21l) shows excellent in vitro efficacies with EC50s of 7.03 nM and 11.8 nM for β-arrestin recruitment and internalization, respectively[1].

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

S1P1 agonist 5 相关抗体:
体内研究
(In Vivo)

S1P1 agonist 5 shows good oral bioavaliabily in rats (F=54.2%) and dogs (F=31.8%)[1].
S1P1 agonist 5 (10 mg/kg; p.o.) inhibits the lymphocyte egress from the lymphoid tissue to the peripheral blood and that lymphopenia can be recovered within 24 hours[1].
S1P1 agonist 5 (3, 10 mg/kg, p.o., once daily for 20 days) ameliorates the disease progression and overall severity in EAE mice, showing favorable drug-like properties[1].
Pharmacokinetic Parameters of S1P1 in rats, male beagle dogs[1].

administration parameters rat dog
i.v. T1/2 (h) 1.4±0.3 5.70±1.2
AUC0-∞ (ng*h/mL) 931.3±95.7 14,830.8±5475.4
CL (mL/min/kg) 17.6±2.0 149.9±62.5
Vss (L/kg) 1.7±0.2 828.7±134.2
p.o. Cmax (ng/mL) 1661.1±916.6 3979.4±483.5
Tmax(h) 0.9±0.8 1.3±0.5
T1/2 (h) 1.4±0.2 4.9±0.6
AUC0-∞ (ng*h/mL) 5044.9±1061 23,109.9±7752.2
F (%) 54.2 31.8
Rats, 1 mg/kg for i.v.; 10 mg/kg for p.o.. dogs, 2 mg/kg i.v.;10 mg/kg for p.o.[1]

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

Animal Model: rats, male beagle dogs[1]
Dosage:
Administration: 1 mg/kg for i.v. and 10 mg/kg for p.o (rats); 2 mg/kg for i.v. and 10 mg/kg for p.o.(dogs)
Result: Showed good oral bioavaliabily in rats (F=54.2%) and dogs (F=31.8%).
Animal Model: male wistar rats (5 week, 160-180 g)[1]
Dosage: 10 mg/kg
Administration: p.o.
Result: Inhibited the lymphocyte egress from the lymphoid tissue to the peripheral blood and that lymphopenia can be recovered within 24 hours.
Animal Model: female C57BL/6 mice (10 weeks,19−22 g) (experimental autoimmune encephalitis (EAE) mouse model)[1]
Dosage: 3, 10 mg/kg (dissolved in 2.5% DMSO and 5% Kolliphor HS 15 (Sigma-Aldrich) in distilled water)
Administration: p.o., once daily, 20 days
Result: Ameliorated the disease progression and overall severity in EAE mice, showing favorable drug-like properties.
分子量

450.89

Formula

C23H24ClN2NaO4
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

S1P1 agonist 5 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 *
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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:

S1P1 agonist 52760666-20-2LPL ReceptorLysophospholipid Receptororally activemultiple sclerosis (MS)selectivelymphocyteautoimmune encephalitis (EAE) mouse modeldrug-likeInhibitorinhibitorinhibit

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