EICOSANOID RECEPTOR AGONISTS AND ANTAGONISTS

RA-110
AH-6809
6-Isopropyl-9-xanthone-2-carboxylic acid
99%, MW=298.3, Storage: RT
Selective prostaglandin E₂ receptor (EP1) antagonist. Useful at concentrations up to 10 mM, at which point it starts to block PGD₂ and TXA₂ receptors¹.
5 mg
25 mg

PG-036
13-APA
(?13-Azaprostanoic acid
98%, MW=311.5 [71629-07-7] Storage: -20°C.
A moderately potent, but specific thromboxane A₂ receptor (TP) antagonist. More selective (5-fold) for the platelet (human) versus vascular (rat) TP receptor^2-6.
1 mg
10 mg

PG-035
Carbacyclin
Carbocyclic PGI₂
99%, crystalline solid, MW=350.5 [69552-46-1] Storage: -20°C. A chemically stable carbocyclic analog of prostacyclin having a similar spectrum of activity but with lower (one-tenth) potency. Inhibits platelet aggregation, reduces systemic arterial blood pressure⁷ relaxes coronary arteries, deaggregates platelet clumps and relaxes human respiratory smooth muscles⁹. Platelet aggregation inhibition is markedly enhanced by a phosphodiesterase inhibitor¹⁰. Short duration of action (similar to prostacyclin) is due to its removal from the circulation and enzymatic inactivation¹¹. An excellent mimic of the effects of naturally occurring prostacyclin^12,13.
1 mg
10 mg

RA-106
Cloprostenol·sodium
16-(m-Chlorophenoxy)-tetranor-prostaglandin F_2a sodium salt
98%, MW=446.9 [55028-72-3] Storage: -20°C. Potent FP agonist¹⁴, more potent (2- to 3-fold) than fluprostenol but less selective. Similar in potency to PGF_2a at EP and TP receptors¹.
1 mg
10 mg

LB-014
14,15-Dehydro-leukotriene B₄
50 µg/ml ethanol, 99%, MW=334.5, Storage: -80°C
Leukotriene B₄ antagonist. Inhibits LTB₄ induced lysozyme release (IC₅₀=1 µM)¹⁵.
50 µg
5 x 50 µg

PG-021
16,16-Dimethyl-prostaglandin E₂
99% MW=380.5 [39746-25-3] Storage: -80°C
An antisecretory, antiulcer prostaglandin E₂ analog with potent cytoprotective activity^16-19. Resistant to metabolic inactivation. Useful for in vivo applications. EP receptor agonist, 10-fold more selective for EP₁ than EP₂ receptors^1,20.
1 mg
10 mg

TABLE 10. NOMENCLATURE AND CHARACTERISTICS OF PROSTANOID RECEPTORS

RA-105
Fluprostenol
(?16-(m-Trifluoromethylphenoxy)-tetranor-prostaglandin F₂
98%, solution in ethanol, MW=458.2 [40666-16-8] Storage: -20°C.
Potent FP agonist14, equipotent with PGF_2a but far more selective. Demonstrates no agonist activity at DP, EP, IP, or TP receptors²⁰. Useful tool for identifying FP receptors in mixed receptor populations¹.
1 mg
10 mg

RA-111
ICI-192,605
98%, MW=402.9 [117621-64-4] Storage: -20°C.
A potent and selective, orally active thromboxane A₂ antagonist^21,22.
10 mg
50 mg

LB-704
LTB₄-APA
Leukotriene B₄-3-aminopropylamide
50 µg/ml ethanol, 99%, MW=392.6, Storage: -80°C. A useful affinity label²³ and hapten for antibody production²⁴. Binds to high affinity LTB₄ receptors (K_D=69 nM)²³ and induces receptor desensitization²⁵. May be covalently coupled to radioiodinatable, photoaffinity or fluorescent probes.
50 µg
5 x 50 µg

LB-714
LTB₄-APA-fluorescein
50 µg/ml ethanol, 98%, MW=782.0, Storage: -80°C
A novel fluorescent leukotriene B₄ receptor ligand.
50 µg
5 x 50 µg

EI-102
Leukotriene B₄-dimethyl amide
50 µg/ml ethanol, 99%, MW=363.5 [83024-92-4] Storage: -80°C
Leukotriene B₄ antagonist. Inhibits binding of [³H]-LTB₄ to guinea pig lung membranes (K_i=0.13 µM)²⁶. Antagonizes the degranulation response to LTB₄ in rabbit PMNL (K_D=0.2 µM) acting, most likely, via receptor desensitization. Partial agonist at higher concentrations (5 µM)²⁷.
50 µg
5 x 50 µg

RA-101
LY 171883
98%, MW=318.4 [88107-10-2] Storage: RT
Selective, orally active leukotriene D₄ antagonist²⁸. K_i=0.63 µM for inhibition of [³H]-LTD₄ binding to guinea pig lung membranes²⁹.
10 mg
50 mg

RA-109
MK-571
99%, MW=537.1 [115104-28-4] Storage: -20°C
A potent, selective, orally active leukotriene D₄ antagonist. Ki=2.1 nM for inhibition of [³H]LTD₄ binding to human lung membranes. Competitively antagonizes contractions of guinea pig trachea and ileum and human trachea induced by LTD₄. Blocks LTD₄. and ascaris-induced bronchoconstriction in conscious squirrel monkeys³⁰.
5 mg
25 mg

PG-051
Misoprostol (SC-29333)
(?-15-Deoxy-(16R,S)-16-hydroxy-16-methyl-prostaglandin E₁, methyl ester
99%, MW=382.5 [59122-46-2] Storage: -20°C
A cytoprotective PGE₁ analog. Prevents NSAID-induced gastric ulceration³¹. Misoprostol is a methyl ester and is therefore inactive in receptor preparations and in other situations where it does not undergo in vivo ester hydrolysis.
10 mg
100 mg

PG-052
Misoprostol, free acid
(?-15-Deoxy-(16R,S)-16-hydroxy-16-methyl-prostaglandin E₁
99%, MW=368.5 [59122-46-2] Storage: -20°C
Active in cell culture and receptor preparations.
Inquire

PG-042
17-Phenyl-trinor-prostaglandin E₂
98%, MW=386.5 [38315-43-4] Storage: -20°C
Selective prostaglandin E₂ (EP₁ ) agonist³².
1 mg
10 mg

RA-104
Picotamide
98%, MW=376.2 [32828-81-2] Storage: RT
A dual activity thromboxane A₂ antagonist and TXA₂ synthase inhibitor^33,34,35. Clinically useful antiplatelet agent.
10 mg
50 mg

P-002
PTA₂
Pinane thromboxane A₂
Solution in ethanol, 99%, MW=376.5 [71111-01-8] Storage: -20°C.
A chemically stable, carbocyclic analog of thromboxane A₂. Antagonizes coronary artery contraction (ID₅₀=0.l µM) and platelet aggregation (ID₅₀=2.0 µM) induced by prostaglandin endoperoxide analogs and arachidonic acid^36,37,38. Inhibits thromboxane synthase and protects ischemic myocardium³⁹. Licensed under U.S. patent 4,308,396.
1 mg
10 mg

EI-209
REV-5901
-Pentyl-3-(2-quinolinylmethoxy)-benzenemethanol
98%, MW=335.4, Storage: RT.
A dual activity leukotriene D₄ antagonist (K_i=0.7 µM, inhibition of [³H]-LTD₄ binding to guinea pig lung membranes⁴⁰) and 5-lipoxygenase inhibitor (IC₅₀=6 µM)^41,42.
10 mg
50 mg

RA-112
SC-51322
98%, MW=457.9, Storage: -20°C
A potent and selective prostaglandin E₂ antagonist (pA₂=8.1). Displays in vivo analgesic activity in the mouse (ED₅₀=0.9 mg/kg)⁴³.
5 mg
25 mg

RA-113
SC-51089
98%, MW=459.3 [146033-02-5] Storage: -20°C
A potent and selective prostaglandin E₂ (EP1) antagonist⁴⁴. Displays in vivo analgesic activity in the rat⁴⁵. Does not block PGE₁ induced hyperalgesia⁴⁶.
5 mg
25 mg

RA-103
SQ-29548
99%, MW=387.5 [98299-61-7] Storage: 0°C
Selective thromboxane A₂ antagonist⁴⁷. IC₅₀=12 nM for inhibition of arachidonic acid induced human platelet aggregation⁴⁸. K_i=7.9 nM for inhibition of [³H]-U-46619 binding to human platelet membranes⁴⁹.
1 mg
10 mg

RA-108
BML-111
5(S),6(R),7-Trihydroxyheptanoic acid, methyl ester
99%, MW=192.2, Storage: -20°C.
Potent lipoxin A₄ agonist, equiactive as LXA₄ in inhibition of LTB₄ induced PMNL chemotaxis (IC₅₀=5 nM)⁵⁰.
1 mg
5 mg

PG-023
U-46619
9,11-Dideoxy-9a,11a-methanoepoxy PGF_2a
99% [56985-40-1] MW=350.5, Storage: -20°C.
A chemically stable analog of PGH₂ which acts as a selective thromboxane A₂ (TP) receptor agonist. A very useful, stable thromboxane A₂ mimetic^36,51,52.
1 mg
10 mg

RA-102
U-75302
99%, MW=361.5 [119477-85-9] Storage: -80°C
Selective leukotriene B₄ antagonist⁵³, K_i=159 nM for inhibition of [³H]-LTB₄ binding to guinea pig lung membranes²⁶.
100 mg
5 x 100 mg

REFERENCES

1. R.A. Coleman In Prostaglandins and Related Substances; A Practical Approach, C. Benedetto, R.G. McDonald-Gibson, S. Nigam and T.F. Slater (eds.) IRL Press, Oxford and Washington D.C. 1987 p. 267

2. G.C. LeBreton et al. Proc. Natl. Acad. Sci. USA 1979 76 4097

3. P.T. Horn et al. J. Cardiovasc. Pharmacol. 1984 6 609

4. S.C. Hung et al. Biochim. Biophys. Acta 1983 728 171

5. L.V. Parise et al. Thromb. Res. 1982 28 721

6. E.J. Kattelman et al. Thromb. Res. 1986 41 471

7. B. Whittle, Jr. et al. Prostaglandins 1980 19 605

8. R. Ceserani et al. Prostaglandins Med. 1980 5 131

9. P.G. Adaikan et al. Prostaglandins Med. 1980 5 307

10. A. Morita et al. Life Sci. 1980 27 695

11. J.W. Aiken et al. Prostaglandins 1980 19 629

12. S.M.M. Karim et al. Prostaglandins Med. 1981 6 521

13. B. Whittle, Jr. et al. Circulation 1985 72 1219

14. M. Dukes et al. Nature 1974 250 330

15. T. Shimazaki et al. Prostaglandins 1990 39 459

16. T. Ohno et al. Gastroenterology 1985 88 353

17. A. Kowalewiski et al. Prostaglandins 1978 15 901

18. B.D. Rush et al. Prostaglandins 1989 37 683

19. N.K. Boughton-Smith and B.J.R. Whittle et al. Prostaglandins 1988 35 945

20. R.A. Coleman et al. In Trends in Autonomic Pharmacology, S. Kalsner (ed.) Taylor and Francis, London and Philadelphia 1985 3 35

21. J.J. Descombes et al. Eur. J. Pharmacol. 1993 243 193

22. N. al Jarad et al. Br. J. Clin. Pharmacol 1994 37 97

23. D.W. Goldman et al. Federation Proc. 1987 46 202

24. R.N. Young et al. Prostaglandins 1983 26 605

25. D. Kiel et al. Adv. Prostagland. Thromboxane Leukotriene Res. 1990 21A 403

26. R.C. Falcone and D. Aharony J. Pharmacol. Exp. Ther. 1990 255 565

27. H.J. Showell et al. Biochem. Biophys. Res. Commun. 1982 106 741

28. J.H. Fleisch et al. J. Pharmacol. Exp. Ther. 1985 233 148

29. D. Aharony et al. J. Pharmacol. Exp. Ther. 1987 243 548

30. T.R. Jones et al. Can. J.Physiol. Pharmacol. 1989 67 17

31. Y. Graham et al. Lancet 1988 2 1277

32. S. Watson and A. Abbott Trends Pharmacol. Sci. 1991 12 suppl. 24

33. P.A. Modesti et al. Eur. J. Pharmacol. 1989 169 85

34. M. Berrettini et al. Eur. J. Clin. Pharmacol. 1990 39 495

35. F. Numano et al. Thromb. Haem. 1989 62 554

36. S.E. Burke et al. Br. J. Pharmac. 1983 78 287

37. A.M. Lefer et al. Proc. Natl. Acad. Sci. USA 1979 76 2566

38. H. Araki et al. Adv. Prostagland. Thromboxane Res. 1980 7 835

39. K. Schrör et al. Amer. J. Physiol. 1980 238 H87

40. R.G. VanInwegen et al. J. Pharmacol. Exp. Ther. 1987 241 117

41. S.M. Coutts et al. In Prostaglandins Leukotrienes and Lipoxins (J.M. Bailey, ed) Plenum, NY 1985 p. 626

42. E.J. Kusner et al. Biochem. Pharmacol. 1989 38 4283

43. E.A. Hallinan et al. Bioorg. Med. Chem. Lett. 1994 4 509

44. E.A. Hallinan et al. J. Med. Chem. 1993 36 3293

45. A.B. Malmberg et al. Neurosci. Lett. 1994 173 193

46. S.G. Khasar et al. Neuroscience 1994 62 345

47. M.L. Ogletree et al. J. Pharmacol. Exp. Ther. 1985 234 435

48. M. Nalane et al. Adv. Prostagland. Thromboxane Res. 1985 15 291

49. E.J. Kattelman et al. Thromb. Res. 1986 41 471

50. T.H. Lee et al. Biochem. Biophys. Res. Commun. 1991 180 1416

51. R.A. Coleman et al. Br. J. Pharmacol. 1981 73 773

52. N. Liel et al. Prostaglandins 1987 33 789

53. A.H. Lin et al. Ann. NY Acad. Sci. 1988 524 196