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MedKoo product information:
Omtriptolide
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MedKoo Code#: 200385
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Name: Omtriptolide
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CAS#: 195883-06-8
(Omtriptolide);
195883-09-1 (Omtriptolide sodium)
Synonym:
PG490-88Na. Chemical name: ***Butanedioic acid,
mono[(3bS,4aS,5aR,6R,6aS,7aS,7bS,8aS,8bS)-1,3,3b,4,4a,6,6a,7a,7b,8b,9,10-
dodecahydro-8b-methyl-6a-(1-methylethyl)-1-oxotrisoxireno[4b,5:6,7:8a,9]phenanthro[1,2-c]furan-6-yl]
ester, sodium salt; ***sodium
4-[(3bS,4aS,5aR,6R,6aS,7aS,7bS,8aS,8bS)-8b-methyl-6a-(1-methylethyl)-1-oxo-1,3,3b,4,4a,6,6a,7a,7b,8b,9,10-dodecahydrotrisoxireno[4b,5:6,7:8a,9]phenanthro[1,2-c]furan-6-yl]-4-oxobutanoate.
IUPAC/Chemical name:
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Chemical structure: |
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Theoretical analysis: |
Chemical Formula: C24H27NaO9
Molecular Weight: 482.45
Elemental Analysis: C, 59.75; H, 5.64; Na, 4.77; O, 29.85 |
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Availability and price:
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Information about this agent
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PG490-88 is a semisynthetic derivative of the novel
compound PG490 (triptolide) purified from a Chinese herb. It has been
shown to prolong acute allograft survival in multiple experimental organ
transplant models. However, the effect of PG490-88 on prevention of
acute and chronic renal allograft rejection has not been determined.
Kidneys of ACI or F344 rats were transplanted into bilaterally
nephrectomized LEW recipients as the acute or chronic allograft
rejection models, respectively. Treatment of LEW recipients with
PG490-88 significantly prolonged ACI kidney graft survival in a
dose-dependent manner when compared with the untreated allograft
controls. LEW recipients of F344 kidney grafts who received PG490-88 for
90 days with a brief course of low-dose FK506 showed normal serum
creatinine levels and markedly reduced histological changes of chronic
rejection at day 90 after transplantation. These results suggest that
PG490-88 significantly prolongs kidney allograft survival in an acute
rejection model and prevents chronic allograft rejection in rats.
See: Transplant Proc. 2005 Jan-Feb;37(1):134-6.
http://www.ncbi.nlm.nih.gov/pubmed/15808572.
Current developer:
Pharmagenesis
1: Chen G, Sun H, Arp J, Garcia B, Wang X, Wise
Y, Liu W, Ramcharran S, Huang X, Xiang Y, Yang H, Fang Z, Madrenas J,
Sudo Y, Tamura K, Zhong R. A synergistic effect between PG490-88 and
tacrolimus prolongs renal allograft survival in monkeys. Am J
Transplant. 2006 Apr;6(4):714-23. Erratum in: Am J Transplant. 2006
Jun;6(6):1498. Madenas, J [corrected to Madrenas, J]. PubMed PMID:
16539628.
2: Wang X, Sun H, Chen G, Liu W, Wise Y, Yung C, Sudo Y, Tamura K,
Garcia B, Zhong R. Immunosuppression with a combination of pg490-88 and
a subtherapeutic dose of FK506 in a canine renal allograft model.
Transplantation. 2005 Jun 15;79(11):1537-44. PubMed PMID: 15940043.
3: Fisniku O, Pan F, Wynn C, Erickson LM, Crews G, Jang MS, Sudo Y,
Tamura K, Kobayashi M, Benediktsson H, Jiang H. Protective effects of
PG490-88 on chronic allograft rejection by changing intragraft gene
expression profiles. Transplant Proc. 2005 May;37(4):1962-4. PubMed
PMID: 15919518.
4: Crews GM, Erickson L, Pan F, Fisniku O, Jang MS, Wynn C, Benediktsson
H, Kobayashi M, Jiang H. Down-regulation of TGF-beta and VCAM-1 is
associated with successful treatment of chronic rejection in rats.
Transplant Proc. 2005 May;37(4):1926-8. PubMed PMID: 15919506.
5: Pan F, Fisniku O, Wynn C, Erickson LM, Crews G, Jang MS, Sudo Y,
Tamura K, Kobayashi M, Benediktsson H, Jiang H. PG490-88, a new
immunosuppressant, effectively prevents acute and chronic rejection in
rat renal allografts. Transplant Proc. 2005 Jan-Feb;37(1):134-6. PubMed
PMID: 15808572.
6: Fidler JM, Li K, Chung C, Wei K, Ross JA, Gao M, Rosen GD. PG490-88,
a derivative of triptolide, causes tumor regression and sensitizes
tumors to chemotherapy. Mol Cancer Ther. 2003 Sep;2(9):855-62. PubMed
PMID: 14555704.
7: Leonard CT, Soccal PM, Berry GJ, Doyle RL, Theodore J, Duncan SR,
Rosen GD. PG490-88, a derivative of triptolide, attenuates obliterative
airway disease in a mouse heterotopic tracheal allograft model. J Heart
Lung Transplant. 2002 Dec;21(12):1314-8. PubMed PMID: 12490278.
8: Fidler JM, Ku GY, Piazza D, Xu R, Jin R, Chen Z. Immunosuppressive
activity of the Chinese medicinal plant Tripterygium wilfordii. III.
Suppression of graft-versus-host disease in murine allogeneic bone
marrow transplantation by the PG27 extract. Transplantation. 2002 Aug
27;74(4):445-57. PubMed PMID: 12352901.
9: Kiviharju TM, Lecane PS, Sellers RG, Peehl DM. Antiproliferative and
proapoptotic activities of triptolide (PG490), a natural product
entering clinical trials, on primary cultures of human prostatic
epithelial cells. Clin Cancer Res. 2002 Aug;8(8):2666-74. PubMed PMID:
12171899.
10: Chen BJ, Chen Y, Cui X, Fidler JM, Chao NJ. Mechanisms of tolerance
induced by PG490-88 in a bone marrow transplantation model.
Transplantation. 2002 Jan 15;73(1):115-21. PubMed PMID: 11792990.
11: Krishna G, Liu K, Shigemitsu H, Gao M, Raffin TA, Rosen GD.
PG490-88, a derivative of triptolide, blocks bleomycin-induced lung
fibrosis. Am J Pathol. 2001 Mar;158(3):997-1004. PubMed PMID: 11238047;
PubMed Central PMCID: PMC1850337.
12: Chen BJ, Liu C, Cui X, Fidler JM, Chao NJ. Prevention of
graft-versus-host disease by a novel immunosuppressant, PG490-88,
through inhibition of alloreactive T cell expansion. Transplantation.
2000 Nov 27;70(10):1442-7. PubMed PMID: 11118087.
13: Wang J, Xu R, Jin R, Chen Z, Fidler JM. Immunosuppressive activity
of the Chinese medicinal plant Tripterygium wilfordii. I. Prolongation
of rat cardiac and renal allograft survival by the PG27 extract and
immunosuppressive synergy in combination therapy with cyclosporine.
Transplantation. 2000 Aug 15;70(3):447-55. PubMed PMID: 10949186.
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