2. Apoptosis
  3. TNF Receptor
  4. Balinatunfib

Balinatunfib  (Synonyms: SAR-441566; TNFα activity modulator 3)

Cat. No.: HY-160412 Purity: 98.40%
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COA
Handling Instructions Technical Support

Balinatunfib (SAR-441566) is an orally active inhibitor of TNFR1 signaling. By binding to the central pocket of the soluble TNFα (sTNFα) trimer, Balinatunfib stabilizes an asymmetric conformation, blocking its binding to TNFR1 (without affecting TNFR2) and thus inhibiting downstream pathways. Balinatunfib has anti-inflammatory activity, and can be used in the study of autoimmune diseases.

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

Balinatunfib Chemical Structure

Balinatunfib Chemical Structure

CAS No. : 2248726-53-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

Balinatunfib Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

Balinatunfib (SAR-441566) is an orally active inhibitor of TNFR1 signaling. By binding to the central pocket of the soluble TNFα (sTNFα) trimer, Balinatunfib stabilizes an asymmetric conformation, blocking its binding to TNFR1 (without affecting TNFR2) and thus inhibiting downstream pathways. Balinatunfib has anti-inflammatory activity, and can be used in the study of autoimmune diseases[1][2].

In Vitro

Balinatunfib (1-1000 nM; 4 h) efficiently inhibits the expression of CD11b on granulocytes activated by Zymosan (HY-159069) in human whole blood, with an IC50 of 35 nM and an IC90 of 163 nM[2].

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

Balinatunfib Related Antibodies
In Vivo

Balinatunfib (1-30 mg/kg; oral administration; twice daily; 20 days) exerts improvement effects in a mouse arthritis model[2].
Pharmacokinetic Analysis in Male Animals[2]

Species Route Dose (mg/kg) tmax (h) Cmax (ng/mL) AUCinf (ng.h/mL) CL (L/h/kg) Vz (L/kg) T1/2,z (h) Bioavailability (%)
Rat i.v. 1 / 424 731 1.38 4.1 2.1 /
Rat p.o. 3 4 73.6 573 / / / 26
Dog i.v. 1 / 1510 4200 0.267 2.68 7.00 /
Dog p.o. 30 2 6920 131000 / / / 108
Dog p.o. 100 7 6320 258000 / / / 62
Cynomolgus monkey i.v. 1 / 774 2970 0.355 2.59 6.66 /
Cynomolgus monkey p.o. 3 2 609 6620 / / / 67
Cynomolgus monkey p.o. 10 6 1250 20000 / / / 68
Cynomolgus monkey p.o. 20 8 2490 45200 / / / 77
Cynomolgus monkey p.o. 100 6 3640 107000 / / / 36

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

Animal Model: Male DBA/1 mice treated Collagen (HY-NP113)[2]
Dosage: 1, 3, 10 and 30 mg/kg
Administration: Oral administration; twice daily; 20 days
Result: Showed a dose-dependent inhibition of arthritis symptoms. The 10 mg/kg dose group reduced the AUC of the disease score by 68%, and the 30 mg/kg dose group reduced it by 84%.
Protected the joint bone and improved bone microstructure parameters at doses of 10 mg/kg and 30 mg/kg.
Molecular Weight

502.52

Formula

C27H24F2N6O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC(F)OC1=C(C(C2=O)=CC=C1)[C@](C[C@@]3([H])N2C)([H])N4C3=NC5=CC=C(C6=CN=C(C7(CCC7)N)N=C6)C=C45
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 : 116.67 mg/mL (232.17 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 1.9900 mL 9.9499 mL 19.8997 mL
5 mM 0.3980 mL 1.9900 mL 3.9799 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.40%

SDS (252 KB)

COA (259 KB) HNMR (271 KB) LCMS (99 KB)

Handling Instructions (2659 KB)
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 1.9900 mL 9.9499 mL 19.8997 mL 49.7493 mL
5 mM 0.3980 mL 1.9900 mL 3.9799 mL 9.9499 mL
10 mM 0.1990 mL 0.9950 mL 1.9900 mL 4.9749 mL
15 mM 0.1327 mL 0.6633 mL 1.3266 mL 3.3166 mL
20 mM 0.0995 mL 0.4975 mL 0.9950 mL 2.4875 mL
25 mM 0.0796 mL 0.3980 mL 0.7960 mL 1.9900 mL
30 mM 0.0663 mL 0.3317 mL 0.6633 mL 1.6583 mL
40 mM 0.0497 mL 0.2487 mL 0.4975 mL 1.2437 mL
50 mM 0.0398 mL 0.1990 mL 0.3980 mL 0.9950 mL
60 mM 0.0332 mL 0.1658 mL 0.3317 mL 0.8292 mL
80 mM 0.0249 mL 0.1244 mL 0.2487 mL 0.6219 mL
100 mM 0.0199 mL 0.0995 mL 0.1990 mL 0.4975 mL
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Balinatunfib 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:

Balinatunfib2248726-53-4SAR-441566 TNFα activity modulator 3SAR441566SAR 441566TNFα activity modulator3TNFα activity modulator 3TNFα activity modulator-3TNF ReceptorTumor Necrosis Factor ReceptorTNFRTNFR1 inhibitorautoimmune diseasesTNFαarthritis modelInhibitorinhibitorinhibit

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