PF-8380
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 503216

CAS#: 1144035-53-9

Description: PF-8380 is a potent autotaxin inhibitor with an IC(50) of 2.8 nM in isolated enzyme assay and 101 nM in human whole blood. PF-8380 has adequate oral bioavailability and exposures required for in vivo testing of autotaxin inhibition. Autotaxin's role in producing LPA in plasma and at the site of inflammation was tested in a rat air pouch model. The specific inhibitor PF-8380 , dosed orally at 30 mg/kg, provided >95% reduction in both plasma and air pouch LPA within 3 h, indicating autotaxin is a major source of LPA during inflammation. At 30 mg/kg PF-8380 reduced inflammatory hyperalgesia with the same efficacy as 30 mg/kg naproxen.


Price and Availability

Size Price Shipping out time Quantity
100mg USD 450 2 Weeks
200mg USD 750 2 Weeks
500mg USD 1450 2 Weeks
1g USD 2250 2 Weeks
2g USD 3950 2 Weeks
5g USD 5950 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-20. Prices are subject to change without notice.

PF-8380, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 503216
Name: PF-8380
CAS#: 1144035-53-9
Chemical Formula: C22H21Cl2N3O5
Exact Mass: 477.08583
Molecular Weight: 478.32
Elemental Analysis: C, 55.24; H, 4.43; Cl, 14.82; N, 8.78; O, 16.72


Synonym: PF8380; PF-8380; PF 8380.

IUPAC/Chemical Name: 3,5-dichlorobenzyl 4-(3-oxo-3-(2-oxo-2,3-dihydrobenzo[d]oxazol-6-yl)propyl)piperazine-1-carboxylate

InChi Key: JMSUDQYHPSNBSN-UHFFFAOYSA-N

InChi Code: InChI=1S/C22H21Cl2N3O5/c23-16-9-14(10-17(24)12-16)13-31-22(30)27-7-5-26(6-8-27)4-3-19(28)15-1-2-18-20(11-15)32-21(29)25-18/h1-2,9-12H,3-8,13H2,(H,25,29)

SMILES Code: O=C(N1CCN(CCC(C2=CC=C3NC(OC3=C2)=O)=O)CC1)OCC4=CC(Cl)=CC(Cl)=C4


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
soluble in DMSO

Shelf Life:
>5 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001


Additional Information

  
  
 
 


References

1: Szepanowski F, Derksen A, Steiner I, Meyer Zu Hörste G, Daldrup T, Hartung HP, Kieseier BC. Fingolimod promotes peripheral nerve regeneration via modulation of lysophospholipid signaling. J Neuroinflammation. 2016 Jun 10;13(1):143. doi: 10.1186/s12974-016-0612-9. PubMed PMID: 27283020; PubMed Central PMCID: PMC4901498.

2: Velasco M, O'Sullivan C, Sheridan GK. Lysophosphatidic acid receptors (LPARs): Potential targets for the treatment of neuropathic pain. Neuropharmacology. 2016 Apr 5. pii: S0028-3908(16)30129-0. doi: 10.1016/j.neuropharm.2016.04.002. [Epub ahead of print] Review. PubMed PMID: 27059127.

3: Katsifa A, Kaffe E, Nikolaidou-Katsaridou N, Economides AN, Newbigging S, McKerlie C, Aidinis V. The Bulk of Autotaxin Activity Is Dispensable for Adult Mouse Life. PLoS One. 2015 Nov 16;10(11):e0143083. doi: 10.1371/journal.pone.0143083. eCollection 2015. PubMed PMID: 26569406; PubMed Central PMCID: PMC4646642.

4: Navab M, Chattopadhyay A, Hough G, Meriwether D, Fogelman SI, Wagner AC, Grijalva V, Su F, Anantharamaiah GM, Hwang LH, Faull KF, Reddy ST, Fogelman AM. Source and role of intestinally derived lysophosphatidic acid in dyslipidemia and atherosclerosis. J Lipid Res. 2015 Apr;56(4):871-87. doi: 10.1194/jlr.M056614. Epub 2015 Feb 2. PubMed PMID: 25646365; PubMed Central PMCID: PMC4373744.

5: Bhave SR, Dadey DY, Karvas RM, Ferraro DJ, Kotipatruni RP, Jaboin JJ, Hallahan AN, Dewees TA, Linkous AG, Hallahan DE, Thotala D. Autotaxin Inhibition with PF-8380 Enhances the Radiosensitivity of Human and Murine Glioblastoma Cell Lines. Front Oncol. 2013 Sep 17;3:236. doi: 10.3389/fonc.2013.00236. eCollection 2013. PubMed PMID: 24062988; PubMed Central PMCID: PMC3775313.

6: Salous AK, Panchatcharam M, Sunkara M, Mueller P, Dong A, Wang Y, Graf GA, Smyth SS, Morris AJ. Mechanism of rapid elimination of lysophosphatidic acid and related lipids from the circulation of mice. J Lipid Res. 2013 Oct;54(10):2775-84. doi: 10.1194/jlr.M039685. Epub 2013 Aug 15. PubMed PMID: 23948545; PubMed Central PMCID: PMC3770090.

7: St-Cœur PD, Ferguson D, Morin P Jr, Touaibia M. PF-8380 and closely related analogs: synthesis and structure-activity relationship towards autotaxin inhibition and glioma cell viability. Arch Pharm (Weinheim). 2013 Feb;346(2):91-7. doi: 10.1002/ardp.201200395. Epub 2013 Jan 8. PubMed PMID: 23300119.

8: Gierse J, Thorarensen A, Beltey K, Bradshaw-Pierce E, Cortes-Burgos L, Hall T, Johnston A, Murphy M, Nemirovskiy O, Ogawa S, Pegg L, Pelc M, Prinsen M, Schnute M, Wendling J, Wene S, Weinberg R, Wittwer A, Zweifel B, Masferrer J. A novel autotaxin inhibitor reduces lysophosphatidic acid levels in plasma and the site of inflammation. J Pharmacol Exp Ther. 2010 Jul;334(1):310-7. doi: 10.1124/jpet.110.165845. Epub 2010 Apr 14. PubMed PMID: 20392816.