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  3. (R)-HM5023507

(R)-HM5023507 是一种潜在的 PI3K 抑制剂。(R)-HM5023507 可用于癌症、炎症性疾病、过敏性疾病、自身免疫性疾病和白血病等疾病的相关研究。

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(R)-HM5023507

(R)-HM5023507 Chemical Structure

CAS No. : 1549740-86-4

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

(R)-HM5023507 is a potential PI3K inhibitor. (R)-HM5023507 can be used for the research of cancer, inflammatory, allergic and autoimmune diseases and leukemia etc[1].

IC50 & Target

PI3Kγ

4 nM (IC50)

PI3Kδ

5 nM (IC50)

PI3Kβ

590 nM (IC50)

PI3Kα

3960 nM (IC50)

PI3Kγ

0.6 nM (Kd)

PI3Kδ

2.43 nM (Kd)

PI3Kβ

640 nM (Kd)

PI3Kα

2420 nM (Kd)

药代动力学
(Parmacokinetics)
Species Dose Route F Half-life Clearance (CL) Vss
Rat[1] 2.5 mg/kg i.v. / 5.1 h 3.3 mL/min/kg 1.2 L/kg
Rat[1] 10 mg/kg p.o. 104 % / / /
体内研究
(In Vivo)
Animal Model: Female Wistar rats (4-6 weeks old) were orally dosed with the compound for blood samples collection[1].
Dosage: 0.01 mg/kg; 0.03 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: p.o.; single dose
Result: Attenuated PI3K δ/γ-mediated immune signaling in the rat in a dose-related manner.
Animal Model: Female Wistar rats (4-6 weeks old) were orally dosed with the compound for blood samples collection[1].
Dosage: 0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: p.o.; single dose
Result: Attenuated the neutrophil chemotaxis in a dose-related manner, with a clear trend for reduction seen at a dose of 3 mg/kg and a reduction to baseline levels at 10 mg/kg.
Animal Model: Female Wistar rats (4-6 weeks old) were injected with Con-A (30 mg/kg; i.v.) for an inflammatory model[1].
Dosage: 0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: p.o.; single dose
Result: Decreased IFNγ levels in a dose- and exposure-related manner.
Inhibited plasma IFNγ >80% at a dose of 10 mg/kg.
Animal Model: Female Wistar rats (4-6 weeks old) were intradermally injected with bovine type II collagen (200 μg) at the base of the tail on days 0 and 6 for an arthritis model[1].
Dosage: 0.1 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg
Administration: p.o.; BID
Result: Attenuated arthritic paw inflammation.
Improved histopathology- and micro-computed tomography (µCT)-based indices of joint damage, bone destruction.
Attenuated the levels of anti-collagen antibody.
Animal Model: Female Wistar rats (4-6 weeks old) were intradermally injected with bovine type II collagen (200 μg) at the base of the tail on days 0 and 6 for an arthritis model[1].
Dosage: 0.6 mg/kg; 6 mg/kg
Administration: p.o.; QD
Result: Attenuated arthritic paw inflammation.
Improved histopathology- and micro-computed tomography (µCT)-based indices of joint damage, bone destruction.
Attenuated the levels of anti-collagen antibody.
分子量

435.87

Formula

C21H18ClN7O2

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
  • 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.

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产品名称:
(R)-HM5023507
目录号:
HY-177277A
需求量: