DA-1241

DA-1241
Identifiers
	IUPAC name 3-[4-[3-[1-(5-Ethylpyrimidin-2-yl)piperidin-4-yl]propoxy]-2,6-difluorophenyl]-5-propan-2-yl-1,2,4-oxadiazole;
PubChem CID	121304331;
Chemical and physical data
Formula	C25H31F2N5O2
Molar mass	471.553 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CCC1=CN=C(N=C1)N1CCC(CCCOC2=CC(F)=C(C3=NOC(=N3)C(C)C)C(F)=C2)CC1;
	InChI InChI=1S/C25H31F2N5O2/c1-4-17-14-28-25(29-15-17)32-9-7-18(8-10-32)6-5-11-33-19-12-20(26)22(21(27)13-19)23-30-24(16(2)3)34-31-23/h12-16,18H,4-11H2,1-3H3; Key:XQSZLXRXPGLHLH-UHFFFAOYSA-N;

DA-1241 is an experimental GPR119 receptor agonist developed by the South Korean company Dong-A ST for non-alcoholic steatohepatitis and type 2 diabetes.^[1]^[2]^[3]^[4]

References edit

^ Lee, Seung-Ho; Park, Hansu; Yang, Eun-Kyoung; Lee, Bo Ram; Jung, Il-Hoon; Kim, Tae-Hyoung; Goo, Moon Jung; Chae, Yuna; Kim, Mi-Kyung (October 2023). "GPR119 activation by DA-1241 alleviates hepatic and systemic inflammation in MASH mice through inhibition of NFκB signaling". Biomedicine & Pharmacotherapy. 166: 115345. doi:10.1016/j.biopha.2023.115345. PMID 37657264.
^ Kim, Mi-Kyung; Cheong, Ye Hwang; Lee, Seung Ho; Kim, Tae Hyoung; Jung, Il Hoon; Chae, Yuna; Lee, Jeong-Ha; Yang, Eun Kyoung; Park, Hansu; Yang, Jae-Sung; Hong, Ki Whan (December 2021). "A novel GPR119 agonist DA-1241 preserves pancreatic function via the suppression of ER stress and increased PDX1 expression". Biomedicine & Pharmacotherapy. 144: 112324. doi:10.1016/j.biopha.2021.112324.
^ Kim, Mi-Kyung; Lee, Dae Young; Jeong, Jiyoon; Grimm, Michael; Franey, Bridgette B.; Hompesch, Marcus (1 June 2021). "766-P: DA-1241, a Novel GPR119 Agonist: Data on Safety, Tolerability, and Pharmacokinetics (PK) from Part 1 of a Phase 1b Multiple Ascending Dose (MAD) Study in Healthy Volunteers (HV)". Diabetes. 70 (Supplement_1). doi:10.2337/db21-766-P. S2CID 237883271.
^ Kim, Youjin; Lee, Si Woo; Wang, Hyejin; Kim, Ryeong-Hyeon; Park, Hyun Ki; Lee, Hangkyu; Kang, Eun Seok (31 March 2022). "DA-1241, a Novel GPR119 Agonist, Improves Hyperglycaemia by Inhibiting Hepatic Gluconeogenesis and Enhancing Insulin Secretion in Diabetic Mice". Diabetes & Metabolism Journal. 46 (2): 337–348. doi:10.4093/dmj.2021.0056. PMC 8987681. PMID 35052026.

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[1] Lee, Seung-Ho; Park, Hansu; Yang, Eun-Kyoung; Lee, Bo Ram; Jung, Il-Hoon; Kim, Tae-Hyoung; Goo, Moon Jung; Chae, Yuna; Kim, Mi-Kyung (October 2023). "GPR119 activation by DA-1241 alleviates hepatic and systemic inflammation in MASH mice through inhibition of NFκB signaling". Biomedicine & Pharmacotherapy. 166: 115345. doi:10.1016/j.biopha.2023.115345. PMID 37657264.

[2] Kim, Mi-Kyung; Cheong, Ye Hwang; Lee, Seung Ho; Kim, Tae Hyoung; Jung, Il Hoon; Chae, Yuna; Lee, Jeong-Ha; Yang, Eun Kyoung; Park, Hansu; Yang, Jae-Sung; Hong, Ki Whan (December 2021). "A novel GPR119 agonist DA-1241 preserves pancreatic function via the suppression of ER stress and increased PDX1 expression". Biomedicine & Pharmacotherapy. 144: 112324. doi:10.1016/j.biopha.2021.112324.

[3] Kim, Mi-Kyung; Lee, Dae Young; Jeong, Jiyoon; Grimm, Michael; Franey, Bridgette B.; Hompesch, Marcus (1 June 2021). "766-P: DA-1241, a Novel GPR119 Agonist: Data on Safety, Tolerability, and Pharmacokinetics (PK) from Part 1 of a Phase 1b Multiple Ascending Dose (MAD) Study in Healthy Volunteers (HV)". Diabetes. 70 (Supplement_1). doi:10.2337/db21-766-P. S2CID 237883271.

[4] Kim, Youjin; Lee, Si Woo; Wang, Hyejin; Kim, Ryeong-Hyeon; Park, Hyun Ki; Lee, Hangkyu; Kang, Eun Seok (31 March 2022). "DA-1241, a Novel GPR119 Agonist, Improves Hyperglycaemia by Inhibiting Hepatic Gluconeogenesis and Enhancing Insulin Secretion in Diabetic Mice". Diabetes & Metabolism Journal. 46 (2): 337–348. doi:10.4093/dmj.2021.0056. PMC 8987681. PMID 35052026.

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[2]

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Identifiers

IUPAC name 3-[4-[3-[1-(5-Ethylpyrimidin-2-yl)piperidin-4-yl]propoxy]-2,6-difluorophenyl]-5-propan-2-yl-1,2,4-oxadiazole
PubChem CID	121304331
Chemical and physical data
Formula	C₂₅H₃₁F₂N₅O₂
Molar mass	471.553 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES CCC1=CN=C(N=C1)N1CCC(CCCOC2=CC(F)=C(C3=NOC(=N3)C(C)C)C(F)=C2)CC1
InChI InChI=1S/C25H31F2N5O2/c1-4-17-14-28-25(29-15-17)32-9-7-18(8-10-32)6-5-11-33-19-12-20(26)22(21(27)13-19)23-30-24(16(2)3)34-31-23/h12-16,18H,4-11H2,1-3H3 Key:XQSZLXRXPGLHLH-UHFFFAOYSA-N