2. Immunology/Inflammation
  3. PGE synthase
  4. HPGDS inhibitor 3

HPGDS inhibitor 3 是一种具有口服活性且高效的外周限制性造血前列腺素 D 合成酶 (H-PGDS) 抑制剂，IC50 为 9.4 nM，EC50 为 42 nM。HPGDS inhibitor 3 具有良好的选择性，在小鼠、大鼠和犬体内的药动学参数良好，且无中枢神经系统毒性。HPGDS inhibitor 3 具有抗炎活性。

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HPGDS inhibitor 3 Chemical Structure

HPGDS inhibitor 3 Chemical Structure

CAS No. : 2255311-93-2

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HPGDS inhibitor 3 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HPGDS inhibitor 3 is an orally active and highly potent peripherally restricted hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with IC50 value of 9.4 nM and EC50 of 42 nM, respectively. HPGDS inhibitor 3 exhibits good selectivity, good pharmacokinetic parameters in mouse, rat, and dog, and no CNS toxicity. HPGDS inhibitor 3 has anti-inflammatory activity[1].

IC50 & Target

IC50: 9.4 nM (H-PGDS)[1]
EC50: 42 nM (H-PGDS)[1]
体内研究
(In Vivo)

HPGDS inhibitor 3 (compound 1y) (1-3 mg/kg; PO and IV; single) has a lower IV clearance, similar steady state volume of distribution, longer terminal half-life, and high oral bioavailability, as well as very low brain exposures in mouse, rat and dog[1].
HPGDS inhibitor 3 (0.003-1 mg/kg; PO; single) attenuates PGD2 release to baseline levels in a dose-dependent manner; also inhibits LPS-induced PGD2 increase in plasma and skeletal muscle in a dose-dependent manner[1].
HPGDS inhibitor 3 (0.003-1 mg/kg; PO; single) [1].
HPGDS inhibitor 3 (1, 3, and 10 mg/kg; PO; q.d., for 16 days) significantly enhances functional recovery of injured limbs, and hastens the time to full functional recovery of injured limb muscles[1].
HPGDS inhibitor 3 (10, 30 and 100 mg/kg; PO; once daily, for 7 days or 4 days) exhibits well tolerated at 30 mg/kg/day in rat but not tolerated at 100 mg/kg/day; shows well tolerated at 30 mg/kg/day in dogs but not tolerated at 75 mg/kg/day[1].
Pharmacokinetic Parameters of HPGDS inhibitor 3 in mice, rats and dogs[1].

Mouse
IV, 1 mg/kg
PO, 3 mg/kg		 Rat
IV, 0.4 mg/kg
PO, 2.4 mg/kg		 Dog
IV, 0.5 mg/kg
PO, 1 mg/kg
T1/2 (h) 2.9 5.1 6.2
CL (mL/min/kg) 9.0 4.5 1.9
Vss (L/kg) 1.6 1.6 1.0
F (%) 71 100 92
Brain:blood ratio 0.06

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

Animal Model: Male C57BL/6J mice (murine mast cell degranulation model of inflammation)[1]
Dosage: 0.003, 0.01, 0.03, 0.1, 0.3 and 1.0 mg/kg
Administration: PO; single (anesthetized 1 hour later, intraperitoneally injected with 0.2 mL PBS or 48/80 (0.75 mg/mL))
Result: Attenuated PGD2 release to baseline levels in a dose-dependent manner with an ED50 of 0.009 mg/kg (blood EC50 = 3.4 nM) in this acute inflammation model.
Animal Model: Male C57BL6/N mice (12 weeks, n=6)[1]
Dosage: 0.003, 0.01, 0.03, 0.1, 0.3 and 1.0 mg/kg
Administration: PO; single (intraperitoneally injection of PBS or 20 ng/kg LPS 1 hour later)
Result: Inhibited LPS-induced PGD2 increase in plasma and skeletal muscle in a dose-dependent manner.
Animal Model: Male C57Bl/6 mice (10-12 weeks, n=7-8; chronic eccentric contraction-induced muscle injury models)[1]
Dosage: 1, 3, and 10 mg/kg
Administration: PO; q.d., for 16 days
Result: Significantly enhanced functional recovery of injured limbs, and significantly hastened the time to full functional recovery of injured limb muscles, with maximal efficacy observed at ≥ 10 mg/kg q.d..
Animal Model: Mdx mouse (6-8 mouths, duchenne muscular dystrophy model)[1]
Dosage: 0.1, 0.3, 1, 3, and 10 mg/kg
Administration: PO; q.d., for 43 days
Result: Significantly improved functional recovery (~90% to 100% restoration), following eccentric contraction-induced muscle injury in mdx mice.
Animal Model: Male Wistar Han rat and dog[1]
Dosage: 10, 30 and 100 mg/kg for rat; 10, 30, and 75 mg/kg for dog
Administration: PO; once daily; for 7 days (rat) or for 4 days (dog)
Result: In rat, the AUC values at 10, 30, and 100 mg/kg/day were 120, 410, and 820 µg•hr/mL, respectively; respective Cmax values were 8.7, 24, and 57 μg/mL. In dog, it showed well tolerated at dose levels up to 30 mg/kg/day with no abnormal microscopic findings; but exhibited discoloration in the small intestine and esophagus (female) at 75 mg/kg/day.
Animal Model: Mice, rats, dongs[1]
Dosage: 1 mg/kg IV and 3 mg/kg p.o in mice, 0.4 mg/kg IV and 2.4 mg/kg PO in rat, 0.5 mg/kg IV and 1 mg/kg PO in dog
Administration: IV and PO; single (Pharmacokinetics Analysis)
Result: Had a lower IV clearance, similar steady state volume of distribution, longer terminal half-life, and high oral bioavailability, as well as very low brain exposures in mouse, rat and dog.
分子量

353.46

Formula

C21H27N3O2
CAS 号
非同位 CAS

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

HPGDS inhibitor 3 相关分类

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  • 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:

HPGDS inhibitor 32255311-93-2HPGDS inhibitor3HPGDS inhibitor-3PGE synthaseProstaglandin E synthaseOrally activitySelectivityPharmacokineticAnti-inflammatoryInhibitorinhibitorinhibit

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