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

JPE-1375 Estructura química

No. CAS : 1254036-23-1

Tamaño Precio Stock Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 En stock
Solution
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Based on 4 publication(s) in Google Scholar

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Descripciòn

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
Peso molecular

955.08

Fòrmula

C49H63FN10O9
No. CAS
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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

4°C, protect from light

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

Solvente y solubilidad
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.

  • Calculadora de molaridad

  • Calculadora de dilución

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Pureza y Documentación

Purity: 99.96%

SDS (252 KB)

COA (255 KB) RP-HPLC (221 KB) MS (70 KB)

Instrucciones de manejo (2659 KB)
Referencias

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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  • 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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Nombre del producto:
JPE-1375
Cat. No.:
HY-148141
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