2. Immunology/Inflammation
  3. NOD-like Receptor (NLR)
  4. Usnoflast

Usnoflast is the selective, orally active inhibitor for NLRP3 that blocks the release of IL-1β, and exhibits anti-inflammatory activity.

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

Usnoflast

Usnoflast Chemical Structure

CAS No. : 2455519-86-3

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Based on 1 publication(s) in Google Scholar

Usnoflast Related Antibodies

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Description

Usnoflast is the selective, orally active inhibitor for NLRP3 that blocks the release of IL-1β, and exhibits anti-inflammatory activity[1][2].

IC50 & Target

NLRP3[1]
In Vitro

Usnoflast inhibits Nigericin (HY-127019)-induced IL-1β release in THP-1 cells, ATP (HY-B2176)-mediated IL-1β release in human PBMCs, and Nigericin (HY-127019)-mediated IL-1β release in primary mouse microglia, IC50s are 11 nM, 4.5 nM and 43 nM, respectively[2].
Usnoflast inhibits the oligomerization of caspase recruitment domain (ASC), interfere with the formation of NLRP3 inflammasome complex[2].

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

Usnoflast Related Antibodies
In Vivo

Usnoflast (2.5-10 mg/kg, po, single dose) reduces the levels of IL-1β and caspase-1 in the brain tissue of mice, exhibits anti-inflammatory activity in LPS (HY-D1056)-induced encephalitis model[2].
Usnoflast (10-60 mg/kg, po, twice daily for 5 weeks) improves the motor dysfunction of mice, and reduces the abnormal accumulation of α-synuclein in MPTP (HY-15608)-induced Parkinson's disease model[2].

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

Animal Model: MPTP (HY-15608)-induced mouse Parkinson's disease model[2]
Dosage: 10-60 mg/kg
Administration: po, twice daily for 5 weeks
Result: Improved the motor dysfunction of mice, reduced the abnormal accumulation of α-synuclein, increased the number of tyrosine hydroxylase (TH)-positive dopaminergic neurons.
Molecular Weight

403.54

Formula

C21H29N3O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@]1(N(CCC1)C)/C=C/S(NC(NC2=C3C(CCC3)=CC4=C2CCC4)=O)(=O)=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 : 62.5 mg/mL (154.88 mM; ultrasonic and warming and heat to 60°C; 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 2.4781 mL 12.3903 mL 24.7807 mL
5 mM 0.4956 mL 2.4781 mL 4.9561 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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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 2.4781 mL 12.3903 mL 24.7807 mL 61.9517 mL
5 mM 0.4956 mL 2.4781 mL 4.9561 mL 12.3903 mL
10 mM 0.2478 mL 1.2390 mL 2.4781 mL 6.1952 mL
15 mM 0.1652 mL 0.8260 mL 1.6520 mL 4.1301 mL
20 mM 0.1239 mL 0.6195 mL 1.2390 mL 3.0976 mL
25 mM 0.0991 mL 0.4956 mL 0.9912 mL 2.4781 mL
30 mM 0.0826 mL 0.4130 mL 0.8260 mL 2.0651 mL
40 mM 0.0620 mL 0.3098 mL 0.6195 mL 1.5488 mL
50 mM 0.0496 mL 0.2478 mL 0.4956 mL 1.2390 mL
60 mM 0.0413 mL 0.2065 mL 0.4130 mL 1.0325 mL
80 mM 0.0310 mL 0.1549 mL 0.3098 mL 0.7744 mL
100 mM 0.0248 mL 0.1239 mL 0.2478 mL 0.6195 mL
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Usnoflast 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:

Usnoflast2455519-86-3NOD-like Receptor (NLR)Parkinson's diseaseTHP-1selectiveorally activeInhibitorinhibitorinhibit

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