PM 102Antagonist of heparin CAS# 1234564-95-4 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 1234564-95-4 | SDF | Download SDF |
PubChem ID | 90488905 | Appearance | Powder |
Formula | C235H425N111O64 | M.Wt | 5829.6 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Solubility | Soluble to 5 mg/ml in water | ||
Sequence | AEARARRAAARAARRAKK(AEARARRAAAR (Modifications: Ala-1 = N-terminal Ac, Ala-19 = ε-Ac, X-36 = Dpr, Ala-37 = β-Ac, Glu-53 = C-terminal Amide) | ||
Chemical Name | (4S)-4-[[3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamidopropanoyl]amino]-4-carboxybutanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]propanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-2-[[(2S)-1-[(2S)-6-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamidopropanoyl]amino]-4-carboxybutanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]propanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamidopropanoyl]amino]-4-carboxybutanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]propanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-6-aminohexanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]propanoyl]amino]-5-amino-5-oxopentanoic acid | ||
SMILES | CC(C(=O)NC(CCC(=O)O)C(=O)NC(C)C(=O)NC(CCCNC(=N)N)C(=O)NC(C)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCCNC(=N)N)C(=O)NC(C)C(=O)NC(C)C(=O)NC(C)C(=O)NC(CCCNC(=N)N)C(=O)NC(C)C(=O)NC(C)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCCNC(=N)N)C(=O)NC(C)C(=O)NCCCCC(C(=O)N1CCCC1C(=O)NC(CNC(=O)C(C)NC(=O)C(CCCNC(=N)N)NC(=O)C(CCCNC(=N)N)NC(=O)C(C)NC(=O)C(C)NC(=O)C(CCCNC(=N)N)NC(=O)C(C)NC(=O)C(C)NC(=O)C(C)NC(=O)C(CCCNC(=N)N)NC(=O)C(CCCNC(=N)N)NC(=O)C(C)NC(=O)C(CCCNC(=N)N)NC(=O)C(C)NC(=O)C(CCC(=O)O)NC(=O)C(C)NC(=O)C)C(=O)NC(CCC(=O)O)C(=O)N)NC(=O)C(CCCCN)NC(=O)C(C)NC(=O)C(CCCNC(=N)N)NC(=O)C(CCCNC(=N)N)NC(=O)C(C)NC(=O)C(C)NC(=O)C(CCCNC(=N)N)NC(=O)C(C)NC(=O)C(C)NC(=O)C(C)NC(=O)C(CCCNC(=N)N)NC(=O)C(CCCNC(=N)N)NC(=O)C(C)NC(=O)C(CCCNC(=N)N)NC(=O)C(C)NC(=O)C(CCC(=O)O)NC(=O)C(C)NC(=O)C)NC(=O)C | ||
Standard InChIKey | WRMCCUFFCSYBDM-YUELKKPWSA-N | ||
Standard InChI | InChI=1S/C235H425N111O64/c1-105(306-199(392)143(62-41-91-281-224(250)251)338-208(401)149(68-47-97-287-230(262)263)329-183(376)122(18)303-174(367)116(12)308-193(386)137(56-35-85-275-218(238)239)323-180(373)119(15)300-168(361)110(6)297-171(364)113(9)311-201(394)145(64-43-93-283-226(254)255)340-211(404)152(71-50-100-290-233(268)269)332-190(383)126(22)314-196(389)140(59-38-88-278-221(244)245)326-187(380)129(25)318-205(398)155(76-80-162(352)353)335-177(370)107(3)294-132(28)347)166(359)274-84-34-32-55-158(344-214(407)136(54-31-33-83-236)322-186(379)125(21)317-204(397)148(67-46-96-286-229(260)261)343-210(403)151(70-49-99-289-232(266)267)331-185(378)124(20)305-176(369)118(14)310-195(388)139(58-37-87-277-220(242)243)325-182(375)121(17)302-170(363)112(8)299-173(366)115(11)313-203(396)147(66-45-95-285-228(258)259)342-213(406)154(73-52-102-292-235(272)273)334-192(385)128(24)316-198(391)142(61-40-90-280-223(248)249)328-189(382)131(27)320-207(400)157(78-82-164(356)357)337-179(372)109(5)296-134(30)349)217(410)346-103-53-74-160(346)216(409)345-159(215(408)321-135(165(237)358)75-79-161(350)351)104-293-167(360)106(2)307-200(393)144(63-42-92-282-225(252)253)339-209(402)150(69-48-98-288-231(264)265)330-184(377)123(19)304-175(368)117(13)309-194(387)138(57-36-86-276-219(240)241)324-181(374)120(16)301-169(362)111(7)298-172(365)114(10)312-202(395)146(65-44-94-284-227(256)257)341-212(405)153(72-51-101-291-234(270)271)333-191(384)127(23)315-197(390)141(60-39-89-279-222(246)247)327-188(381)130(26)319-206(399)156(77-81-163(354)355)336-178(371)108(4)295-133(29)348/h105-131,135-160H,31-104,236H2,1-30H3,(H2,237,358)(H,274,359)(H,293,360)(H,294,347)(H,295,348)(H,296,349)(H,297,364)(H,298,365)(H,299,366)(H,300,361)(H,301,362)(H,302,363)(H,303,367)(H,304,368)(H,305,369)(H,306,392)(H,307,393)(H,308,386)(H,309,387)(H,310,388)(H,311,394)(H,312,395)(H,313,396)(H,314,389)(H,315,390)(H,316,391)(H,317,397)(H,318,398)(H,319,399)(H,320,400)(H,321,408)(H,322,379)(H,323,373)(H,324,374)(H,325,375)(H,326,380)(H,327,381)(H,328,382)(H,329,376)(H,330,377)(H,331,378)(H,332,383)(H,333,384)(H,334,385)(H,335,370)(H,336,371)(H,337,372)(H,338,401)(H,339,402)(H,340,404)(H,341,405)(H,342,406)(H,343,403)(H,344,407)(H,345,409)(H,350,351)(H,352,353)(H,354,355)(H,356,357)(H4,238,239,275)(H4,240,241,276)(H4,242,243,277)(H4,244,245,278)(H4,246,247,279)(H4,248,249,280)(H4,250,251,281)(H4,252,253,282)(H4,254,255,283)(H4,256,257,284)(H4,258,259,285)(H4,260,261,286)(H4,262,263,287)(H4,264,265,288)(H4,266,267,289)(H4,268,269,290)(H4,270,271,291)(H4,272,273,292)/t105-,106-,107-,108-,109-,110-,111-,112-,113-,114-,115-,116-,117-,118-,119-,120-,121-,122-,123-,124-,125-,126-,127-,128-,129-,130-,131-,135-,136-,137-,138-,139-,140-,141-,142-,143-,144-,145-,146-,147-,148-,149-,150-,151-,152-,153-,154-,155-,156-,157-,158-,159?,160-/m0/s1 | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
Description | Peptide that reverses the anticoagulant effect of heparin. Potently binds heparin (Kd = 36 nM in vitro). |
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Reversal of heparin-induced increases in aPTT in the rat by PM102, a novel heparin antagonist.[Pubmed:20307530]
Eur J Pharmacol. 2010 Jun 10;635(1-3):165-70.
Protamine is the only agent approved to reverse heparin-induced anticoagulation. Due to the significant adverse effects of protamine there is an important need for an alternative agent with an improved safety profile. The pharmacodynamics of PM102, a novel peptide-based heparin antagonist, was evaluated and compared to protamine in a rat model. Rats were dosed with intravenous heparin (50U/kg) and 4min later with protamine (0.25, 0.75mg/kg single intravenous bolus) or PM102 (0.1, 0.3, 1, 3, 30mg/kg single intravenous bolus). Blood samples were collected though 60min for assessment of activated partial thromboplastin time (aPTT) and plasma concentration of PM102. Both doses of protamine markedly lowered the elevated aPTT to baseline values within 1 to 5min after administration. PM102 (0.3-30mg/kg) also rapidly and completely reversed heparin-induced increases in aPTT within 1 to 5min. The effects of PM102 administered as an infusion over 10min also reversed aPTT with similar potency to that observed for bolus administration. The onset of reversal with infusion was delayed relative to the same total dose given as a bolus; however, the maximum effect was similar. PM102 rapidly (T(max) 1-2.6min) appeared in plasma after dosing. Concentrations of PM102 generally declined rapidly after reaching T(max) with a mean T(1/2) of 4 to 31min. PM102 is a novel synthetic peptide that effectively reverses the anticoagulant effect of heparin. It's utility as a bolus injection as well as infusion, its rapid efficacy and its rapid clearance make this an ideal candidate for clinical development.