1. Immunology/Inflammation
  2. Interleukin Related
  3. Navepdekinra

Navepdekinra  (Synonyms: DC-806; LY4100504; S-011806)

Cat. No.: HY-153780 Purity: 98.58%
Handling Instructions Technical Support

Navepdekinra (DC-806) is an orally active, potent interleukin-17A (IL-17A) inhibitor (IC50 = 10.81 nM). Navepdekinra disrupts the IL-17A protein-receptor interaction, suppressing the downstream pro-inflammatory signaling pathway. Navepdekinra inhibits arthritis in a collage-induced arthritis (CIA) rat model. Navepdekinra can be used for psoriasis, psoriatic arthritis, and ankylosing spondylitis[1][2][3].

For research use only. We do not sell to patients.

Navepdekinra

Navepdekinra Chemical Structure

CAS No. : 2467732-66-5

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Based on 1 publication(s) in Google Scholar

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Description

Navepdekinra (DC-806) is an orally active, potent interleukin-17A (IL-17A) inhibitor (IC50 = 10.81 nM). Navepdekinra disrupts the IL-17A protein-receptor interaction, suppressing the downstream pro-inflammatory signaling pathway. Navepdekinra inhibits arthritis in a collage-induced arthritis (CIA) rat model. Navepdekinra can be used for psoriasis, psoriatic arthritis, and ankylosing spondylitis[1][2][3].

IC50 & Target[1]

IL-17A

 

In Vitro

Navepdekinra (1 μM, 0-60 min) shows metabolic stability in rat liver microsomes (RLM) but exhibits moderate metabolic clearance in human liver microsomes (HLM)[3].

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

Parmacokinetics[3]
Species Dose Route Indicator value
Rat 25 mg/kg p.o. T1/2 2.66 h
Rat 25 mg/kg p.o. Tmax 0.75 h
Rat 25 mg/kg p.o. Cmax 614 ng/mL
Rat 25 mg/kg p.o. AUCinf 1869 ng·h/mL
In Vivo

Navepdekinra (25 mg/kg, p.o., b.i.d. for 9 days) inhibits arthritis in a CIA rat model[3].

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

Animal Model: Male Wistar rats (6 weeks old) intradermally injected with emulsified Collagen II (CII) in Complete Freund's Adjuvant (CFA) on both day 0 and day 7[3]
Dosage: 25 mg/kg
Administration: p.o., b.i.d. for 9 days
Result: Showed 28.10 % inhibition of arthritis.
Molecular Weight

625.78

Formula

C33H48FN7O4

CAS No.
Appearance

Solid

Color

white

SMILES

O=C(C1=CC=NN1CC)N[C@@H]([C@@]2([H])CC[C@@H](CC2)C)C(NC3=C(C=C(C=C3)[C@H](C)[C@@H](NC(CC)=O)C(N4CCN(CC4)C)=O)F)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (159.80 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 1.5980 mL 7.9900 mL 15.9801 mL
5 mM 0.3196 mL 1.5980 mL 3.1960 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. 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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In Vivo Dissolution Calculator
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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. 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 1.5980 mL 7.9900 mL 15.9801 mL 39.9501 mL
5 mM 0.3196 mL 1.5980 mL 3.1960 mL 7.9900 mL
10 mM 0.1598 mL 0.7990 mL 1.5980 mL 3.9950 mL
15 mM 0.1065 mL 0.5327 mL 1.0653 mL 2.6633 mL
20 mM 0.0799 mL 0.3995 mL 0.7990 mL 1.9975 mL
25 mM 0.0639 mL 0.3196 mL 0.6392 mL 1.5980 mL
30 mM 0.0533 mL 0.2663 mL 0.5327 mL 1.3317 mL
40 mM 0.0400 mL 0.1998 mL 0.3995 mL 0.9988 mL
50 mM 0.0320 mL 0.1598 mL 0.3196 mL 0.7990 mL
60 mM 0.0266 mL 0.1332 mL 0.2663 mL 0.6658 mL
80 mM 0.0200 mL 0.0999 mL 0.1998 mL 0.4994 mL
100 mM 0.0160 mL 0.0799 mL 0.1598 mL 0.3995 mL
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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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Navepdekinra
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HY-153780
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