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ROR gamma-t-IN-1

Product Name
ROR gamma-t-IN-1
CAS No.
1426802-50-7
Chemical Name
ROR gamma-t-IN-1
Synonyms
GSK805;GSK805 ，S6767;ROR gamma-t-IN-1;GSK805 (GSK-805);GSK805, 10 mM in DMSO;RORγt Inverse Agonist II, GSK805;RORγt Inverse Agonist II, GSK805;GSK805,N-(2,6-Dichloro-2'-(trifluoromethoxy)biphenyl-4-yl)-;4-[4-[(dimethylamino)methyl]-3,5-dimethoxyphenyl]-2-methyl-2,7-naphthyridin-1(2H)-one;N-(2,6-dichloro-2'-(trifluoromethoxy)biphenyl-4-yl)-2-(4-(ethylsulfonyl)phenyl)acetamide
CBNumber
CB13048666
Molecular Formula
C23H18Cl2F3NO4S
Formula Weight
532.36
MOL File
1426802-50-7.mol
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ROR gamma-t-IN-1 Property

Boiling point:
617.1±55.0 °C(Predicted)
Density 
1.434±0.06 g/cm3(Predicted)
storage temp. 
2-8°C
solubility 
DMF:3.0(Max Conc. mg/mL);5.64(Max Conc. mM)
DMSO:68.33(Max Conc. mg/mL);128.36(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:2):0.3(Max Conc. mg/mL);0.56(Max Conc. mM)
Ethanol:50.0(Max Conc. mg/mL);93.92(Max Conc. mM)
form 
A crystalline solid
pka
12.33±0.70(Predicted)
color 
White to off-white
InChIKey
CEICQMBWAQAIQX-UHFFFAOYSA-N
SMILES
C1(CC(NC2=CC(Cl)=C(C3=CC=CC=C3OC(F)(F)F)C(Cl)=C2)=O)=CC=C(S(CC)(=O)=O)C=C1
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
5.31369
Product name
RORγt Inverse Agonist II, GSK805
Packaging
10 mg
Price
$267
Updated
2025/07/31
Cayman Chemical
Product number
9002444
Product name
GSK805
Purity
≥98%
Packaging
1mg
Price
$44
Updated
2024/03/01
Cayman Chemical
Product number
9002444
Product name
GSK805
Purity
≥98%
Packaging
5mg
Price
$151
Updated
2024/03/01
Cayman Chemical
Product number
9002444
Product name
GSK805
Purity
≥98%
Packaging
10mg
Price
$235
Updated
2024/03/01
ChemScene
Product number
CS-5079
Product name
GSK805
Purity
97.14%
Packaging
5mg
Price
$160
Updated
2021/12/16
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ROR gamma-t-IN-1 Chemical Properties,Usage,Production

Description

GSK805 is a potent, orally bioavailable retinoid-related orphan receptor gamma t (RORγt) inverse agonist that interacts with the receptor''s putative ligand binding domain without exerting significant effects on DNA binding. It inhibits the expression of IL-17 (at 0.5 μM) in naïve CD4+ T cells activated under Th17-cell-polarizing conditions and affects the broader RORγt-dependent gene network, inhibiting the development and pathogenic function of Th17 cells. GSK805 significantly reduces the severity of experimental autoimmune encephalomyelitis (EAE), a mouse model of multiple sclerosis, when given orally to the hosts at 10 mg/kg daily beginning at the time of disease induction.

Uses

GSK805 is an orally active and CNS penetrant RORγt inhibitor. GSK805 inhibits RORγ and Th17 cells differentiation with pIC50 values of 8.4 and >8.2. GSK805 inhibits the function of Th17 cells. GSK805 can be used for the research of immunity[1].

in vivo

GSK805 (10 mg/kg; p.o. once per day for 35 days) improves the situation of mice with experimental autoimmune encephalomyelitis (EAE)[2]. GSK805 (30 mg/kg; p.o. once) inhibits Th17 cell responses in EAE mice[2].

Animal Model:C57BL/6 mice were immunized with MOG35–55 plus CFA[2]
Dosage:10 mg/kg
Administration:Oral gavage; 10 mg/kg once per day; for 35 days
Result:Efficiently ameliorated the severity of EAE in mice.
Animal Model:C57BL/6 mice with EAE[2]
Dosage:30 mg/kg
Administration:Oral gavage; 30 mg/kg once
Result:Reduced both IFN-γ-IL-17+ and IFN-γ+IL-17+ T cells without altered the frequency of TNF-α+ T cells in EAE mice.

References

[1] Wang Y, et al. Discovery of Biaryl Amides as Potent, Orally Bioavailable, and CNS Penetrant RORγt Inhibitors. ACS Med Chem Lett. 2015 May 26;6(7):787-792. DOI:10.1021/acsmedchemlett.5b00122
[2] Xiao S, et al. Small-molecule RORγt antagonists inhibit T helper 17 cell transcriptional network by divergent mechanisms. Immunity. 2014 Apr 17;40(4):477-89. DOI:10.1016/j.immuni.2014.04.004

ROR gamma-t-IN-1 Preparation Products And Raw materials

Raw materials

Preparation Products

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ROR gamma-t-IN-1 Suppliers

China 62 United States 6 Global 68
Chengdu DingDang Pharmaceutical Co., Ltd.
Tel
028-86040038 13980902949;
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028-85149890
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market@dingdangchem.com
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China
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Suzhou Chenrui Biotechnology Co. LTD
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17625585511
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qq：1580084073
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1580084073@qq.com
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China
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Haoyuan Chemexpress Co., Ltd.
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021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
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China
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Shanghai Lollane Biological Technology Co.,Ltd.
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021-52996696，15000506266 15000506266
Fax
+86-21-52996696
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China
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Struchem Co., Ltd.
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0512-63009836 18994340901
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0512-63006936
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helen@struchem.com
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Guangzhou QiYun Biotechnology Co., Ltd.
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020-61288194 61288195
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020-61288700
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505721671@qq.com
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China
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Shanghai YuanYe Biotechnology Co., Ltd.
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021-61312847; 18021002903
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QQ:3008007432
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3008007409@qq.com
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China
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Shanghai Chaolan Chemical Technology Center
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021-QQ：65489617 15618227136
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21-5161 9052
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Sales@ATKchemical.com
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China
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9126
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Beijing Solarbio Science & Tecnology Co., Ltd.
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010-50973130 18101056239
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3193328036@qq.com
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Amadis Chemical Company Limited
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571-89925085
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0086-571-89925065
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sales@amadischem.com
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1426802-50-7, ROR gamma-t-IN-1Related Search:

GSK8612 4-[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[(3S)-3-piperidinylmethoxy]-1H-imidazo[4,5-c]pyridin-4-yl]-2-methyl-3-butyn-2-ol 1-(1-(3-methoxyphenyl)-7-propoxyindolizin-3-yl)ethanone GSK8612 GSK6853 2-Cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl-benzoicacid GSK620 GSK591 GSK5959 GSK872

  • ROR gamma-t-IN-1
  • GSK805
  • GSK805 (GSK-805)
  • N-(2,6-dichloro-2'-(trifluoromethoxy)biphenyl-4-yl)-2-(4-(ethylsulfonyl)phenyl)acetamide
  • 4-[4-[(dimethylamino)methyl]-3,5-dimethoxyphenyl]-2-methyl-2,7-naphthyridin-1(2H)-one
  • Benzeneacetamide, N-[2,6-dichloro-2'-(trifluoromethoxy)[1,1'-biphenyl]-4-yl]-4-(ethylsulfonyl)-
  • N-[2,6-Dichloro-2'-(trifluoromethoxy)[1,1'-biphenyl]-4-yl]-4-(ethylsulfonyl)benzeneacetamide
  • N-[3,5-dichloro-4-[2-(trifluoromethoxy)phenyl]phenyl]-2-(4-ethylsulfonylphenyl)acetamide
  • GSK805,N-(2,6-Dichloro-2'-(trifluoromethoxy)biphenyl-4-yl)-
  • N-(2,6-dichloro-2'-(trifluoromethoxy)-[1,1'-biphenyl]-4-yl)-2-(4-(ethylsulfonyl)phenyl)acetamide
  • GSK 805,immunity,RAR-related orphan receptor,Inhibitor,GSK805,inhibit,ROR,oral,CNS penetrant,GSK-805,Th17 cell
  • GSK805, 10 mM in DMSO
  • RORγt Inverse Agonist II, GSK805
  • RORγt Inverse Agonist II, GSK805
  • GSK805 ，S6767
  • 1426802-50-7
  • C23H18Cl2F3NO4S