2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
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  4. RORγt inverse agonist 34

RORγt inverse agonist 34 (compound 5a) is a RORγt inverse agonist with an IC50 of 0.094 μM for RORγt-LBD. RORγt inverse agonist 34 is used for psoriasis research.

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

RORγt inverse agonist 34 Chemical Structure

RORγt inverse agonist 34 Chemical Structure

CAS No. : 2247604-77-7

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RORγt inverse agonist 34 Related Antibodies

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Description

RORγt inverse agonist 34 (compound 5a) is a RORγt inverse agonist with an IC50 of 0.094 μM for RORγt-LBD. RORγt inverse agonist 34 is used for psoriasis research[1].

IC50 & Target[1]

RORγt

0.094 μM (IC50)

In Vitro

RORγt inverse agonist 34 (2h) impacts the recruitment of SRC1 coactivating peptide by RORγt-LBD with an IC50 of 0.094 μM[1].
RORγt inverse agonist 34 inhibits the differentiation of Th17 cells effectively with an IC50 of 1.57 μM[1].
RORγt inverse agonist 34 (1 μM, 1 h) exhibits a half-life of 18 min in mouse liver microsomes [1].
RORγt inverse agonist 34 (2.5 min) inhibits hERG with the IC50 of surpassed 40 μM, showing low toxicity to heart[1].

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

RORγt inverse agonist 34 Related Antibodies
In Vivo

RORγt inverse agonist 34 (100 mg/kg, i.p., daily, 7days) exhibits significant efficacy in ameliorating Imiquimod (HY-B0180) induced psoriatic lesions in mice[1].
RORγt inverse agonist 34 (0.25%-4% ointment, daily, 11 days) exhibits anti-psoriasis effects in Imiquimod (HY-B0180) induced psoriatic mice model[1].
RORγt inverse agonist 34 (4% ointment, transdermal administration, applied to the skin with a force of approximately 50 g ) in plasma reaches its peak at approximately 10 min with 0.075 μg/mL in BALB/c mice [1].
RORγt inverse agonist 34 (10%-20% ointment, daily, 12days) has no significant acute toxicity in BALB/c mice[1].

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

Animal Model: The Imiquimod (HY-B0180) -induced psoriasis model was established with female BALB/c mice aged 8 to 10 weeks. A 2 cm × 3 cm area of hair on the backs of the mice was shaved using a depilatory cream to establish experimental areas. The shaved backs and right ears of the mice were treated with a daily topical dose of 62.5 mg of a commercially available 5% Imiquimod (HY-B0180) from day 1 to day 7. The mice in the normal group had a Vaseline Lanette cream applied as an alternative treatment[1].
Dosage: 100 mg/kg
Administration: i.p.,daily 7days
Result: Demonstrated notable anti-inflammatory properties in the mouse model of psoriasis, with the most prominent effects observed at a dose of 4%.
Demonstrated significant efficacy in mitigating the Lmiquimod (HY-B0180B) -induced abnormal spleen enlargement, which is comparable to the positive control Dexamethasone (HY-14648) by comparing the ratios of splenic weight to body weight among different groups of mice.
Exhibited more significant effects in alleviating ear inflammation compared to the positive control Dexamethasone (HY-14648) (5 mg/kg).
Inhibited the erythema and scaling for the back skinwas essentially comparable to that of Dexamethasone (HY-14648).
Molecular Weight

531.71

Formula

C31H37N3O3S
CAS No.
SMILES

O=S(N1CCCC2=CC(NC3=CC4=C(C=C3)C(CCC4)=O)=CC=C21)(N(CC5=CC=C(C=C5)C(C)(C)C)C)=O
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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RORγt inverse agonist 34 Related Classifications

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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.

Keywords:

RORγt inverse agonist 342247604-77-7RORγt inverse agonist34RORγt inverse agonist-34RORRAR-related orphan receptoranti-inflammatoryTh17 cellsimmunotherapypsoriasisInhibitorinhibitorinhibit

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