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Fasiglifam

CAS No.: 1000413-72-8

Category

Cat.NO.:A690887  Purity:98%

Product Details of Fasiglifam

CAS No. : 1000413-72-8
Formula :

C29H32O7S

M.W :

524.63

SMILES Code :
O=C(O)C[C@@H]1COC2=CC(OCC3=CC(C4=C(C)C=C(OCCCS(=O)(C)=O)C=C4C)=CC=C3)=CC=C12
Synonyms :
Tak-875
MDL No. : MFCD18251445
InChI Key : BZCALJIHZVNMGJ-HSZRJFAPSA-N
Pubchem ID : 24857286

Safety of Fasiglifam

GHS Pictogram:
Signal Word: Warning
Hazard Statements: H302-H315-H319-H335
Precautionary Statements: P261-P305+P351+P338

Related Pathways of Fasiglifam

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line

Concentration Treated Time Description References
HEK293 cells 10 µM 2 hours Evaluate the binding ability of Fasiglifam to GPR40 receptor PMC5917010
CHO-GPR40 cells 5 μM 1 hour To determine agonistic activity of compounds against FFA1 receptor, results showed compounds 4b and 4c activated 80% and 61% receptor activity at 5 μM concentration, respectively PMC6021034
Mouse colonic mucosal cells 300 nM 10–15 minutes To compare the pharmacology of FFA1 and FFA4 agonists, finding selective agonists more potent than GW9508 PMC5715575
Human airway smooth muscle (HASM) cells 10 µM 30 min TAK875 significantly attenuated histamine-induced MLC phosphorylation and cortical tension development, while GW9508 showed little effect. PMC7708129
RIN-m5f cells 30 or 150 mg/mL 48 hours To evaluate the effect of YD on insulin secretion in high-glucose and high-fat injured RIN-m5f cells. Results showed that high concentration YD (150 mg/mL) significantly increased glucose-stimulated insulin secretion (GSIS) levels, similar to the TAK-875 group. PMC10043368
Human liver organoids (HLOs) 3, 10, 30 μM 7 days To evaluate oxidative stress and immune responses induced by TAK-875. Results showed that TAK-875 treatment led to increased ROS formation and significant release of inflammatory cytokines MCP-1 and IL-6. PMC9981852

In Vivo:

Species

Animal Model

Administration Dosage Frequency Description References
Mice GPR40 knockout mice Oral 10 mg/kg Single dose Evaluate the effect of Fasiglifam on blood glucose and insulin levels PMC5917010
SD rats Oral glucose tolerance test Oral 10 mg/kg Single dose Evaluate the effect of HWL-088 on glucose tolerance in rats PMC7174891
ZDF (fa/fa) rats Type 2 diabetic rat model Gavage 10 mg/kg/day Once daily for 10 weeks To evaluate the effect of TAK-875 on blood glucose and insulin secretion in type 2 diabetic rats. Results showed that TAK-875 significantly reduced fasting blood glucose (FBG) and the area under the curve (AUC) of OGTT, and increased the AUC of insulin release test (IRT) and glucose-stimulated insulin secretion (GSIS). PMC10043368
Mice Diabetes model Intraperitoneal injection 27 mg/kg Single dose To evaluate the effect of FFA1 agonist on blood glucose control, finding it improved glucose tolerance PMC5715575
Mice Gpr40 knockout and wild-type mice Oral 30 mg/kg Single dose, evaluated after 30 minutes To assess the effect of GPR40 agonists on plasma GLP-1 and GIP levels. Results showed that Gq+Gs agonists like AM-1638 and AM-5262 significantly increased plasma GLP-1 and GIP levels. PMC4314522
Rats Type 1 diabetes model rats Oral 5 and 10 mg/kg Immediately before glucose load TAK-875 (a GPR40 agonist) did not decrease postprandial blood glucose levels up to 30 min after glucose load. PMC10424117
Collaborative Cross mice Collaborative Cross mice Oral gavage 600 mg/kg Single dose To evaluate the mechanisms of TAK-875-induced liver injury and genetic risk factors in Collaborative Cross mice. Results showed that a single high dose of TAK-875 did not cause overt liver injury, but gene expression profiling revealed transcriptional changes associated with immune response, bile acid homeostasis, oxidative stress, and mitochondrial dysfunction. PMC8936092

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01433393 Diabetes Mellitus Phase 3 Completed Japan

More >>

Kisarazu-shi, Chiba, Japan

Matsuyama-shi, Ehime, Japan

Fukuoka-shi Nishi-ku, Fukuoka, Japan

Kasuga-shi, Fukuoka, Japan

Naka-shi, Ibaragi, Japan

Tsuchiura-shi, Ibaragi, Japan

Takamatsu-shi, Kagawa, Japan

Kyoto-shi Fushimi-ku, Kyoto, Japan

Nagasaki-shi, Nagasaki, Japan

Kashihara-shi, Nara, Japan

Kashiwara-shi, Osaka, Japan

Osaka-shi Tsurumi-ku, Osaka, Japan

Sakai-shi Nishi-ku, Osaka, Japan

Shimotsuke-shi, Tochigi, Japan

Chiyoda-ku, Tokyo, Japan

Itabashi-ku, Tokyo, Japan

Ota-ku, Tokyo, Japan

Shinjuku-ku, Tokyo, Japan

Toshima-ku, Tokyo, Japan Less <<

NCT01585792 Diabetic Patients Phase 3 Completed Japan

More >>

Fukuoka-shi, Fukuoka, Japan

Sumida-ku, Tokyo, Japan Less <<

NCT01007097 Diabetes Mellitus, Type 2 Phase 2 Completed
NCT01433406 Diabetes Mellitus Phase 3 Completed
NCT01414920 Diabetes Mellitus, Type 2 Phase 2 Completed
NCT01433419 Diabetes Mellitus Phase 3 Completed Japan

More >>

Katori-shi, Chiba, Japan

Niihama-shi, Ehime, Japan

Chikushino-shi, Fukuoka, Japan

Fukuoka-shi, Fukuoka, Japan

Onga-gun, Fukuoka, Japan

Yukuhashi-shi, Fukuoka, Japan

Hiroshima-shi, Hiroshima, Japan

Chitose-shi, Hokkaido, Japan

Sapporo-shi, Hokkaido, Japan

Koga-shi, Ibaragi, Japan

Ushiku-shi, Ibaragi, Japan

Chigasaki-shi, Kanagawa, Japan

Kamakura-shi, Kanagawa, Japan

Minamata-shi, Kumamoto, Japan

Yatsushiro-shi, Kumamoto, Japan

Sasebo-shi, Nagasaki, Japan

Kashihara-shi, Nara, Japan

Okinawa-shi, Okinawa, Japan

Izumi-shi, Osaka, Japan

Suita-shi, Osaka, Japan

Fujimi-shi, Saitama, Japan

Shimotsuga-gun, Tochigi, Japan

Komatsushima-shi, Tokushima, Japan

Bunkyo-ku, Tokyo, Japan

Chiyoda-ku, Tokyo, Japan

Mitaka-shi, Tokyo, Japan

Shibuya-ku, Tokyo, Japan

Shinjuku-ku, Tokyo, Japan

Toshima-ku, Tokyo, Japan

Shunan-shi, Yamaguchi, Japan

Ube-shi, Yamaguchi, Japan Less <<

NCT01456195 Diabetes Mellitus, Type 2 Phase 3 Completed
NCT01549964 Glycemic Control Phase 3 Terminated(Due to concerns aboMore >>ut potential liver safety (See Detailed Description)) Less <<
NCT01834274 Diabetes Mellitus, Type 2 Phase 3 Terminated(Due to potential coMore >>ncerns about liver safety (See Detailed Description)) Less <<
NCT01834274 Terminated(Due to potential coMore >>ncerns about liver safety (See Detailed Description)) Less <<
NCT01982253 Type 2 Diabetes Mellitus Phase 2 Terminated(Due to potential coMore >>ncerns about liver safety (See Detailed Description)) Less <<
NCT01982253 Terminated(Due to potential coMore >>ncerns about liver safety (See Detailed Description)) Less <<
NCT01481116 Terminated(Due to potential coMore >>ncerns about liver safety (See Detailed Description)) Less <<
NCT01549964 Terminated(Due to concerns aboMore >>ut potential liver safety (See Detailed Description)) Less <<
NCT02015780 Type 2 Diabetes Mellitus
More >> Chronic Kidney Disease Less <<
Phase 3 Withdrawn(Due to potential conMore >>cerns about liver safety (See Detailed Description)) Less << January 2016
NCT01481116 Diabetes Mellitus, Type 2 Phase 3 Terminated(Due to potential coMore >>ncerns about liver safety (See Detailed Description)) Less <<
NCT01456195 Completed
NCT01829464 Diabetes Phase 3 Terminated(Due to potential coMore >>ncerns about liver safety (See Detailed Description)) Less <<
NCT01829477 Diabetes Mellitus, Type 2 Phase 3 Terminated(Due to potential coMore >>ncerns about liver safety (See Detailed Description)) Less <<
NCT00949091 Diabetes Mellitus, Type 2 Phase 1 Completed
NCT01496443 Pharmacokinetics Phase 1 Completed United States, Texas
More >>

San Antonio, Texas, United States Less <<

NCT01829477 Terminated(Due to potential coMore >>ncerns about liver safety (See Detailed Description)) Less <<
NCT01647542 Type 2 Diabetes Mellitus Phase 3 Terminated(Due to potential coMore >>ncerns about liver safety (See Detailed Description)) Less <<
NCT01647542 Terminated(Due to potential coMore >>ncerns about liver safety (See Detailed Description)) Less <<
NCT01609582 Terminated(Due to potential coMore >>ncerns about liver safety (See Detailed Description)) Less <<
NCT01829464 Terminated(Due to potential coMore >>ncerns about liver safety (See Detailed Description)) Less <<
NCT01609582 Type 2 Diabetes
More >> Cardiovascular Disease Less <<
Phase 3 Terminated(Due to potential coMore >>ncerns about liver safety (See Detailed Description)) Less <<

Protocol

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