| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Vasculotide targets the Tie-2 receptor tyrosine kinase (TEK), which is primarily expressed on endothelial cells. As an angiopoietin-1 mimetic, Vasculotide binds to and activates Tie-2, inducing receptor autophosphorylation. This activation promotes endothelial cell survival, stabilizes vascular endothelial (VE)-cadherin at adherens junctions, and reduces endothelial permeability. Tie-2 activation also inhibits inflammatory signaling and protects against vascular leakage induced by endotoxins (LPS) and other inflammatory stimuli. The PEGylated form of the peptide has enhanced stability and pharmacokinetic properties.
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| ln Vitro |
In vitro, Vasculotide activates Tie-2 phosphorylation in endothelial cells in a concentration-dependent manner. It ameliorates endotoxin-induced endothelial barrier dysfunction, as measured by trans-endothelial electrical resistance (TEER) and FITC-dextran permeability assays. It also promotes angiogenesis in cell-based assays, including endothelial cell tube formation on Matrigel. Vasculotide has anti-inflammatory effects, reducing cytokine production in LPS-stimulated endothelial cells. The peptide has no direct cytotoxic effects on endothelial cells at concentrations up to 100 ug/mL.
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| ln Vivo |
In vivo, Vasculotide promotes angiogenesis in a mouse model of diabetic ulcer, accelerating wound healing. It protects mice from vascular leakage and reduces mortality in murine abdominal sepsis models. Vasculotide also decreases microvascular leakage and improves microcirculatory perfusion in a rat model of hemorrhagic shock. It ameliorates endotoxin-induced lung injury and reduces inflammatory markers. The peptide is an investigational drug candidate for the treatment of sepsis, acute lung injury, diabetic ulcers, and other conditions involving endothelial dysfunction.
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| Enzyme Assay |
Vasculotide is not a standard enzyme inhibitor; its activity is assessed by measuring Tie-2 phosphorylation. Endothelial cells (e.g., human umbilical vein endothelial cells, HUVECs) are seeded in 6-well plates and serum-starved for 2-4 h. Vasculotide (0.1-10 ug/mL) is added for 5-30 min at 37degC. Cells are lysed, and Tie-2 phosphorylation (p-Tie-2) is measured by Western blotting using phospho-specific antibodies (p-Tie-2 Tyr992 or Tyr1106). Total Tie-2 is used as a loading control. AKT and eNOS phosphorylation (downstream signaling) are also measured. For barrier function, endothelial cells are seeded on Transwell inserts, and TEER is measured using an ohmmeter. FITC-dextran (70 kDa) permeability is measured by adding dextran to the upper chamber and sampling the lower chamber over 60 min.
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| Cell Assay |
For angiogenesis assays, HUVECs are seeded on Matrigel-coated 96-well plates (1-2×10⁴ cells/well) in serum-free medium with Vasculotide (0.1-10 ug/mL). After 6-18 h, tube formation is quantified by imaging and measuring total tube length (ImageJ). For proliferation assays, endothelial cells are seeded in 96-well plates, and viability is measured by MTT after 24-48 h. For cytotoxicity, endothelial cells are treated with Vasculotide (1-100 ug/mL) for 24 h, and LDH release is measured.
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| Animal Protocol |
For in vivo efficacy, a diabetic wound healing model is used. Male db/db mice (8-10 weeks old, n=8-10/group) are anesthetized, and full-thickness excisional wounds (0.5 cm2) are created on the dorsal back. Vasculotide (10-50 ug/wound) is injected intradermally around the wound margin or applied topically twice weekly for 7-14 days. Wound area is measured by planimetry daily. Wound tissues are harvested for histology (H&E, Masson‘s trichrome, CD31 immunohistochemistry for angiogenesis). For sepsis models, C57BL/6 mice are injected intraperitoneally with LPS (10 mg/kg) or subjected to cecal ligation and puncture (CLP). Vasculotide (0.1-1 mg/kg) is administered IV or IP 30 min before or after LPS/CLP. Survival is monitored for 7 days. Plasma cytokines (TNF-alpha, IL-6) are measured by ELISA. Lung wet/dry ratio and Evans blue dye extravasation are measured to assess vascular leakage. For hemorrhagic shock, rats are subjected to controlled hemorrhage, and Vasculotide (0.1-1 mg/kg) is administered IV during resuscitation. Microcirculatory perfusion is assessed by intravital microscopy.
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| ADME/Pharmacokinetics |
Vasculotide (MW ~14,000, PEGylated) has an extended plasma half-life due to PEGylation, which reduces renal clearance and proteolytic degradation. Following IV administration (0.1-1 mg/kg), the half-life is estimated to be 2-8 h in rodents. The TFA salt form improves solubility. The peptide is formulated in PBS or saline for in vivo use. For research use, it is stored as a lyophilized powder at -20degC (powder: -20degC for 3 years, 4degC for 2 years; in solvent: -80degC for 1 year, -20degC for 6 months). No detailed PK data is publicly available.
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| Toxicity/Toxicokinetics |
Vasculotide is generally well-tolerated in preclinical studies. At effective doses (0.1-1 mg/kg), no significant adverse effects were reported. No acute toxicity (LD₅0) data is available. As an angiopoietin-1 mimetic that activates Tie-2, it is not expected to have off-target toxicity. Long-term safety studies have not been published. Standard safety precautions for handling peptides apply: use PPE (gloves, lab coat, safety goggles), work in a fume hood, avoid inhalation and skin contact. Not for human consumption.
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| References |
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| Additional Infomation |
Vasculotide TFA is a research-grade Tie-2 activator and angiopoietin-1 mimetic. It is not an FDA-approved drug. It is being investigated as a potential therapeutic for sepsis, acute lung injury, diabetic wound healing, and hemorrhagic shock. Preclinical studies have demonstrated its efficacy in reducing vascular leakage, inflammation, and mortality in sepsis models, and accelerating wound healing in diabetic mice. For research use only, not for diagnostic or therapeutic applications. Storage: powder at -20degC for 3 years, 4degC for 2 years; in solvent at -80degC for 1 year, -20degC for 6 months.
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| Molecular Formula |
C236H333F3N84O62S4
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|---|---|
| Molecular Weight |
5524
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| Related CAS # |
Vasculotide;1359657-45-6
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| Appearance |
Colorless to off-white solid powder
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| SMILES |
C.C.C.C.C.C1C(C(=O)N(C1=O)CCC(=O)NCCOCCOCC(COCCOCCNC(=O)CCN2C(=O)CC(C2=O)SC[C@@H](C(=O)N[C@@H](CC3=CN=CN3)C(=O)NC(CC4=CN=CN4)C(=O)N[C@@H](CC5=CN=CN5)C(=O)NC(CCCNC(=N)N)C(=O)N[C@@H](CC6=CN=CN6)C(=O)NC(CO)C(=O)N[C@@H](CC7=CC=CC=C7)C(=O)O)N)(COCCOCCNC(=O)CCN8C(=O)CC(C8=O)SC[C@@H](C(=O)N[C@@H](CC9=CN=CN9)C(=O)NC(CC1=CN=CN1)C(=O)N[C@@H](CC1=CN=CN1)C(=O)NC(CCCNC(=N)N)C(=O)N[C@@H](CC1=CN=CN1)C(=O)NC(CO)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)O)N)COCCOCCNC(=O)CCN1C(=O)CC(C1=O)SC[C@@H](C(=O)N[C@@H](CC1=CN=CN1)C(=O)NC(CC1=CN=CN1)C(=O)N[C@@H](CC1=CN=CN1)C(=O)NC(CCCNC(=N)N)C(=O)N[C@@H](CC1=CN=CN1)C(=O)NC(CO)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)O)N)SC[C@@H](C(=O)N[C@@H](CC1=CN=CN1)C(=O)NC(CC1=CN=CN1)C(=O)N[C@@H](CC1=CN=CN1)C(=O)NC(CCCNC(=N)N)C(=O)N[C@@H](CC1=CN=CN1)C(=O)NC(CO)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)O)N.C(=O)(C(F)(F)F)O
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| InChi Key |
LLFSWDZISOFHGZ-UBKDHYSHSA-N
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| InChi Code |
InChI=1S/C229H312N84O60S4.C2HF3O2.5CH4/c230-145(189(326)286-153(61-129-81-242-109-266-129)201(338)298-161(69-137-89-250-117-274-137)205(342)294-157(65-133-85-246-113-270-133)197(334)282-149(25-13-33-262-225(234)235)193(330)290-165(73-141-93-254-121-278-141)209(346)306-173(97-314)213(350)302-169(221(358)359)57-125-17-5-1-6-18-125)101-374-177-77-185(322)310(217(177)354)41-29-181(318)258-37-45-366-49-53-370-105-229(106-371-54-50-367-46-38-259-182(319)30-42-311-186(323)78-178(218(311)355)375-102-146(231)190(327)287-154(62-130-82-243-110-267-130)202(339)299-162(70-138-90-251-118-275-138)206(343)295-158(66-134-86-247-114-271-134)198(335)283-150(26-14-34-263-226(236)237)194(331)291-166(74-142-94-255-122-279-142)210(347)307-174(98-315)214(351)303-170(222(360)361)58-126-19-7-2-8-20-126,107-372-55-51-368-47-39-260-183(320)31-43-312-187(324)79-179(219(312)356)376-103-147(232)191(328)288-155(63-131-83-244-111-268-131)203(340)300-163(71-139-91-252-119-276-139)207(344)296-159(67-135-87-248-115-272-135)199(336)284-151(27-15-35-264-227(238)239)195(332)292-167(75-143-95-256-123-280-143)211(348)308-175(99-316)215(352)304-171(223(362)363)59-127-21-9-3-10-22-127)108-373-56-52-369-48-40-261-184(321)32-44-313-188(325)80-180(220(313)357)377-104-148(233)192(329)289-156(64-132-84-245-112-269-132)204(341)301-164(72-140-92-253-120-277-140)208(345)297-160(68-136-88-249-116-273-136)200(337)285-152(28-16-36-265-228(240)241)196(333)293-168(76-144-96-257-124-281-144)212(349)309-176(100-317)216(353)305-172(224(364)365)60-128-23-11-4-12-24-128;3-2(4,5)1(6)7;;;;;/h1-12,17-24,81-96,109-124,145-180,314-317H,13-16,25-80,97-108,230-233H2,(H,242,266)(H,243,267)(H,244,268)(H,245,269)(H,246,270)(H,247,271)(H,248,272)(H,249,273)(H,250,274)(H,251,275)(H,252,276)(H,253,277)(H,254,278)(H,255,279)(H,256,280)(H,257,281)(H,258,318)(H,259,319)(H,260,320)(H,261,321)(H,282,334)(H,283,335)(H,284,336)(H,285,337)(H,286,326)(H,287,327)(H,288,328)(H,289,329)(H,290,330)(H,291,331)(H,292,332)(H,293,333)(H,294,342)(H,295,343)(H,296,344)(H,297,345)(H,298,338)(H,299,339)(H,300,340)(H,301,341)(H,302,350)(H,303,351)(H,304,352)(H,305,353)(H,306,346)(H,307,347)(H,308,348)(H,309,349)(H,358,359)(H,360,361)(H,362,363)(H,364,365)(H4,234,235,262)(H4,236,237,263)(H4,238,239,264)(H4,240,241,265);(H,6,7);5*1H4/t145-,146-,147-,148-,149?,150?,151?,152?,153-,154-,155-,156-,157-,158-,159-,160-,161?,162?,163?,164?,165-,166-,167-,168-,169-,170-,171-,172-,173?,174?,175?,176?,177?,178?,179?,180?,229?;;;;;;/m0....../s1
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| Chemical Name |
(2S)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-[[(2R)-2-amino-3-[1-[3-[2-[2-[3-[2-[2-[3-[3-[(2R)-2-amino-3-[[(2S)-1-[[1-[[(2S)-1-[[5-carbamimidamido-1-[[(2S)-1-[[1-[[(1S)-1-carboxy-2-phenylethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-oxopropyl]sulfanyl-2,5-dioxopyrrolidin-1-yl]propanoylamino]ethoxy]ethoxy]-2,2-bis[2-[2-[3-[3-[(2R)-2-amino-3-[[(2S)-1-[[1-[[(2S)-1-[[5-carbamimidamido-1-[[(2S)-1-[[1-[[(1S)-1-carboxy-2-phenylethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-oxopropyl]sulfanyl-2,5-dioxopyrrolidin-1-yl]propanoylamino]ethoxy]ethoxymethyl]propoxy]ethoxy]ethylamino]-3-oxopropyl]-2,5-dioxopyrrolidin-3-yl]sulfanylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoic acid;methane;2,2,2-trifluoroacetic acid
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| Synonyms |
Vasculotide (TFA); Vasculotide TFA
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~25 mg/mL (with ultrasonication)
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| 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
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] 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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.1810 mL | 0.9051 mL | 1.8103 mL | |
| 5 mM | 0.0362 mL | 0.1810 mL | 0.3621 mL | |
| 10 mM | 0.0181 mL | 0.0905 mL | 0.1810 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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