PeptideDB

Parstatin (mouse) 1065756-01-5

Parstatin (mouse) 1065756-01-5

CAS No.: 1065756-01-5

Parstatin(mouse) is a cell-penetrating/penetrable peptide agonist of the PAR-1 thrombin receptor and a potent angiogenes
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Parstatin(mouse) is a cell-penetrating/penetrable peptide agonist of the PAR-1 thrombin receptor and a potent angiogenesis inhibitor.

Physicochemical Properties


Molecular Formula C189H326N58O57S3
Molecular Weight 4419.16
Exact Mass 4418.362
CAS # 1065756-01-5
Related CAS # Parstatin(mouse) TFA
PubChem CID 131954573
Appearance Typically exists as solid at room temperature
LogP -13.3
Hydrogen Bond Donor Count 65
Hydrogen Bond Acceptor Count 66
Rotatable Bond Count 147
Heavy Atom Count 307
Complexity 10700
Defined Atom Stereocenter Count 0
InChi Key SVAINNLHALEEHP-UHFFFAOYSA-N
InChi Code

InChI=1S/C189H326N58O57S3/c1-29-98(22)144(240-165(284)119(76-94(14)15)226-161(280)115(72-90(6)7)224-153(272)104(40-30-58-203-185(193)194)214-152(271)105(41-31-59-204-186(195)196)218-171(290)128-45-35-63-243(128)136(258)80-209-149(268)103(190)56-68-306-27)178(297)237-141(95(16)17)176(295)212-99(23)147(266)223-113(70-88(2)3)150(269)208-79-135(257)213-114(71-89(4)5)160(279)233-125(85-251)169(288)227-117(74-92(10)11)164(283)236-127(87-305)151(270)210-81-137(259)244-64-36-46-129(244)172(291)228-118(75-93(12)13)162(281)225-116(73-91(8)9)163(282)234-126(86-252)170(289)235-123(83-249)166(285)216-106(42-32-60-205-187(197)198)157(276)239-143(97(20)21)183(302)247-67-39-49-132(247)174(293)220-110(57-69-307-28)156(275)232-124(84-250)168(287)221-111(50-53-133(191)255)181(300)245-65-37-47-130(245)173(292)219-109(52-55-139(262)263)155(274)231-122(82-248)167(286)217-108(51-54-138(260)261)154(273)215-107(43-33-61-206-188(199)200)158(277)242-145(101(25)253)179(298)229-120(78-140(264)265)159(278)211-100(24)148(267)241-146(102(26)254)180(299)238-142(96(18)19)177(296)230-121(77-134(192)256)182(301)246-66-38-48-131(246)175(294)222-112(184(303)304)44-34-62-207-189(201)202/h88-132,141-146,248-254,305H,29-87,190H2,1-28H3,(H2,191,255)(H2,192,256)(H,208,269)(H,209,268)(H,210,270)(H,211,278)(H,212,295)(H,213,257)(H,214,271)(H,215,273)(H,216,285)(H,217,286)(H,218,290)(H,219,292)(H,220,293)(H,221,287)(H,222,294)(H,223,266)(H,224,272)(H,225,281)(H,226,280)(H,227,288)(H,228,291)(H,229,298)(H,230,296)(H,231,274)(H,232,275)(H,233,279)(H,234,282)(H,235,289)(H,236,283)(H,237,297)(H,238,299)(H,239,276)(H,240,284)(H,241,267)(H,242,277)(H,260,261)(H,262,263)(H,264,265)(H,303,304)(H4,193,194,203)(H4,195,196,204)(H4,197,198,205)(H4,199,200,206)(H4,201,202,207)
Chemical Name

4-[[1-[5-amino-2-[[2-[[2-[[1-[2-[[2-[[2-[[2-[[2-[[2-[[1-[2-[[2-[[2-[[2-[[2-[[2-[[2-[2-[[2-[[2-[[2-[[2-[[2-[[2-[[1-[2-[(2-amino-4-methylsulfanylbutanoyl)amino]acetyl]pyrrolidine-2-carbonyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-3-methylpentanoyl]amino]-3-methylbutanoyl]amino]propanoylamino]-4-methylpentanoyl]amino]acetyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylpentanoyl]amino]-3-sulfanylpropanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]-4-methylsulfanylbutanoyl]amino]-3-hydroxypropanoyl]amino]-5-oxopentanoyl]pyrrolidine-2-carbonyl]amino]-5-[[1-[[1-[[1-[[1-[[1-[[1-[[1-[[1-[[4-amino-1-[2-[(4-carbamimidamido-1-carboxybutyl)carbamoyl]pyrrolidin-1-yl]-1,4-dioxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-5-oxopentanoic acid
HS Tariff Code 2934.99.9001
Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


ln Vitro LVDP recovery is enhanced by parstatin (0–10 µM) in a concentration-dependent way. LVDP has a 23% recovery rate and an ideal concentration of 1 µM [2].
ln Vivo Pastatin (single dosage, 1-25 µg/kg, intravenously) administered before ischemia shows rapid cardioprotective effects via engaging Gi protein-activated pathways including p38 MAPK, ERK1/2, NOS, and KATP channels. Patatin exerts effects on both cardiomyocytes and the coronary circulation, hence producing cardioprotection. This shows that patatin has a potential therapeutic role in the treatment of heart injury caused by ischemia and reperfusion [1].
Animal Protocol Animal/Disease Models: 8weeks old male SD (SD (Sprague-Dawley)) rats (250-300 g) [1].
Doses: 1-25 mcg/kg.
Route of Administration: Inject intravenously (iv) (iv)(iv) 15 minutes before ischemia.
Experimental Results: Doses of 5-15 µg/kg Dramatically diminished infarct size, with 10 µg/kg being the optimal dose. The infarct size of these hearts accounted for 46 ± 3% of the risk area, which was a 26% reduction compared with the control group.
References

[1]. Parstatin, the Cleaved Peptide on Proteinase-Activated Receptor 1 Activation, Is a Potent Inhibitor of Angiogenesis. J Pharmacol Exp Ther. 2009 Feb;328(2):378-89.

[2]. Parstatin: A Cryptic Peptide Involved in Cardioprotection After Ischaemia and Reperfusion Injury. Cardiovasc Res. 2009 Jul 15;83(2):325-34.


Solubility Data


Solubility (In Vitro) May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
Solubility (In Vivo) Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

Injection Formulations
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO 400 μLPEG300 50 μL Tween 80 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300:Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL Saline)

Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).
Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 0.2263 mL 1.1314 mL 2.2629 mL
5 mM 0.0453 mL 0.2263 mL 0.4526 mL
10 mM 0.0226 mL 0.1131 mL 0.2263 mL
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.