2. Immunology/Inflammation
  3. Complement System
  4. JPE-1375

JPE-1375 is a complement C5a receptor 1 (C5aR1) antagonist. JPE-1375 effectively inhibits polymorphonuclear leukocyte mobilization (EC50=6.9 µM) and reduces TNF levels (EC50=4.5 µM) in mice. JPE-1375 can be used in studies of autoimmune and inflammatory diseases.

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JPE-1375 Chemical Structure

JPE-1375 Chemical Structure

CAS No. : 1254036-23-1

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Based on 1 publication(s) in Google Scholar

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Description

JPE-1375 is a complement C5a receptor 1 (C5aR1) antagonist. JPE-1375 effectively inhibits polymorphonuclear leukocyte mobilization (EC50=6.9 µM) and reduces TNF levels (EC50=4.5 µM) in mice. JPE-1375 can be used in studies of autoimmune and inflammatory diseases[1].

IC50 & Target

C5aR1[1].
In Vivo

JPE-1375 (0.3, 1.0, 3.0 mg/kg; i.v.; single) inhibits PMN (polymorphonuclear leukocytes) mobilization and TNF with EC50 values of 6.9 and 4.5 µM, respectively[1].
JPE-1375 (1 mg/kg; i.v.; single) demonstrates a rapid distribution in the plasma, followed by elimination in mice[1].
JPE-1375 (1 mg/kg; i.v.; single) shows a strong negative correlation between PMN mobilization and TNF production with plasma concentrations[1].

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

Animal Model: C57BL/6J wild-type (10 to 12-week-old; C5a pharmacodynamic model)[1].
Dosage: 0.3, 1.0, 3.0 mg/kg
Administration: Intravenous injection; single.
Result: Significantly decreased C5a-mediated PMN mobilization at 1 and 3 mg/kg doses, while no effect was observed at a 0.3 mg/kg dose.
Showed a significant reduction in TNF plasma levels at 1 and 3 mg/kg dose with both compounds reducing C5a-mediated TNF by about 90%.
Animal Model: C57BL/6J wild-type mice(10 to 12-week-old)[1].
Dosage: 1 mg/kg
Administration: Intravenous injection; single.
Result: 1.19 Pharmacokinetic Parameters of JPE-1375 in C57BL/6J wild-type mice[1].
IV (1 mg/kg)
T1/2 (h) 0.13
Cmax (µg/mL) 7.18
AUC0-t (μg/mL•h) 2.40
AUC0-inf, obs (μg/mL•h) 2.41
AUC0-t/0-inf, obs (μg/mL•h) 1.00
AUMC0-inf, obs (μg/mL•h2) 0.13
MRT0-inf, obs (h) 0.05
Vz, obs ((μg)/(μg/mL)) 2.38
CL, obs ((μg)/(μg/mL)/h) 12.47
Vss, obs ((μg)/(μg/mL)) 0.66
Molecular Weight

955.08

Formula

C49H63FN10O9
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@@H]1CC(NC(N1)=O)=O)N[C@@H](CC2=CC=CC=C2)C(N[C@@H](CCCN)C(N3[C@@H](CCC3)C(N[C@@H](CCC(C)C)C(N[C@H](C(N[C@H](C(N)=O)CC4=CC=CC=C4)=O)CC5=CC=C(C=C5)F)=O)=O)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (104.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0470 mL 5.2352 mL 10.4703 mL
5 mM 0.2094 mL 1.0470 mL 2.0941 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.0470 mL 5.2352 mL 10.4703 mL 26.1758 mL
5 mM 0.2094 mL 1.0470 mL 2.0941 mL 5.2352 mL
10 mM 0.1047 mL 0.5235 mL 1.0470 mL 2.6176 mL
15 mM 0.0698 mL 0.3490 mL 0.6980 mL 1.7451 mL
20 mM 0.0524 mL 0.2618 mL 0.5235 mL 1.3088 mL
25 mM 0.0419 mL 0.2094 mL 0.4188 mL 1.0470 mL
30 mM 0.0349 mL 0.1745 mL 0.3490 mL 0.8725 mL
40 mM 0.0262 mL 0.1309 mL 0.2618 mL 0.6544 mL
50 mM 0.0209 mL 0.1047 mL 0.2094 mL 0.5235 mL
60 mM 0.0175 mL 0.0873 mL 0.1745 mL 0.4363 mL
80 mM 0.0131 mL 0.0654 mL 0.1309 mL 0.3272 mL
100 mM 0.0105 mL 0.0524 mL 0.1047 mL 0.2618 mL
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JPE-1375 Related Classifications

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:

JPE-13751254036-23-1JPE1375JPE 1375Complement SystemPMNTNFautoimmuneinflammatory diseasesInhibitorinhibitorinhibit

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