Transportan
Based on 1 Customer Validation
Transportan is an amphipathic cell-penetrating peptide containing 12 functional amino acids from the amino terminus of the neuropeptide galanin and mastoparan in the carboxyl terminus, connected via a lysine. Transportan interacts with galanin receptors and G-proteins, modulates GTPase activity, enters cells via direct translocation and endocytic pathways, accumulates in cytoplasmic, nuclear, and membranous structures, and delivers cargo including peptides, PNAs, proteins, siRNA, and liposomes[12].
For research use only. We do not sell to patients.
- Purity: 95.25%
- CAS No.: 203716-10-3
- Formula: C134H227N35O32
- Molecular Weight:2840.45
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Storage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Biological Activity
Transportan (10 μM; 30 min/60 h) efficiently penetrates human Bowes melanoma cells at both 0°C and 37°C with comparable high uptake, distributes across the cytoplasm and nucleus, and has an internalization half-time of 3.4 min[1].
Transportan (IC50 22 μM; 12 min at 30 °C) inhibits basal GTPase activity in Rin m5F cellular membranes with an IC50 of 22 μM[1].
Transportan inserts into phospholipid membranes at an oblique 65° angle relative to the surface, spans the bilayer with its mass center 1.7 Å into the first leaflet, and has a 32% α-helical structure in its central region[1].
Transportan (1-10 μM; 1 min to 4 h) exhibits broad, cell-type-independent penetration, localizing to plasma membrane, cytosolic membranes, nuclear membrane, and nucleoli in Bowes’ melanoma cells and other mammalian cell lines, with temperature-dependent differences in intracellular distribution[2].
Transportan binds to galanin receptors in Bowes’ melanoma cell membranes with a Kd value of 17.4 nM[2].
Transportan (0.1 μM-0.1 mM; 12 min) inhibits basal GTPase activity in Bowes’ melanoma cell membranes with an EC50 of 21.1 μM[2].
Transportan (10 μM; 1 h) significantly increases bystander uptake of AgNPs, AuNPs, IONPs, and 70 kDa dextran in CHO-K1, H1975, and HeLa cells, as well as QD uptake in CHO-K1 and H1975 cells, and BSA uptake in CHO-K1 cells[3].
Transportan (10 μM; 1-2 h) induces bystander nanoparticle uptake in CHO-K1 and HeLa cells via receptor-dependent macropinocytosis, with nanoparticles trafficking through early and late endosomes[3].
Transportan (20 μM; 3 h) potently enhances liposome uptake in CHO, H1975, PC3, Neuro2A, Raw 264.7, and primary bone marrow-derived macrophages[4].
Transportan (20 μM; 3 h) enables uptake of hydrophilic probe-loaded liposomes in CHO and H1975 cells[4].
Transportan (20 μM; 3 h)-assisted liposome uptake in CHO cells is mediated primarily by macropinocytosis, with minor contributions from other endocytic pathways[4].
Transportan (10 μM; 60 min at 37 °C) internalizes into human colon cancer Caco-2 cells, localizing to the nuclear membrane, nucleus, and cytoplasm, in an endocytosis-independent manner[5].
Transportan (10 μM; 60 min at 37 °C) induces marked reorganization of actin filaments in confluent human colon cancer Caco-2 cells, producing thicker, more pronounced vertical stress fibres[5].
Transportan (different concentrations; 48 h) co-administration significantly enhances the transfection efficiency of GFP-expressing lentivirus and AAV vectors in PC3 cells, Raw264.7 macrophage cell line, bone marrow-derived macrophages, and retinal pigment epithelium cells when incubated for 48 h, with limited cytotoxicity.
Transportan (TP) (2 μM; 12-48 h) efficiently delivers SASH1 siRNA to HT29 and HCT116 colorectal cancer cells, resulting in significant downregulation of SASH1 mRNA levels.
Fluorescently labeled transportan (0-30 μM; 1 h) shows concentration dependent and nonsaturable cellular uptake in triticale cv AC Alta mesophyll protoplasts, with increased relative fluorescence uptake observed at 5, 10, 20, and 30 μM after 1 h incubation at room temperature[7].
Transportan (320 nmol; 30 h total) delivers functional siNP to inhibit PR8 H1N1 influenza virus replication in MDCK and A549 cells[8].
Transportan (1 μM; 1 h) penetrates the membrane of HeLa human cervical cancer cells but does not enter HEL299 human non-cancer lung fibroblast cells[9].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Transportan (800 nmol; i.v.; single dose) delivers functional siNP to inhibit influenza A virus replication in mice, with 100% survival observed in mice treated with the 50 nmol siNP dose complexed with Transportan[8].
Transportan, as part of a PNA-transportan conjugate targeted to galanin receptor mRNA, regulates galanin receptor levels and modifies pain transmission in rats[11].
Transportan (35-560 µg/kg; i.v.; single bolus injections; 15-minute intervals between escalating doses) induces a dose-dependent reduction in rat systemic blood pressure, with a maximal 35% decrease in mean arterial pressure observed at a dose of 280 µg/kg[12].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 203716-10-3
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Appearance Solid
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Molecular Weight 2840.45
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Formula C134H227N35O32
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Color White to off-white
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Sequence
Gly-Trp-Thr-Leu-Asn-Ser-Ala-Gly-Tyr-Leu-Leu-Gly-Lys-Ile-Asn-Leu-Lys-Ala-Leu-Ala-Ala-Leu-Ala-Lys-Lys-Ile-Leu-NH2
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Sequence Shortening
GWTLNSAGYLLGKINLKALAALAKKIL-NH2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL (35.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (287 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Soomets U, et al. Deletion analogues of transportan. Biochim Biophys Acta. 2000;1467(1):165-176. [Content Brief]
[2]. Pooga M, et al. Cell penetration by transportan. FASEB J. 1998;12(1):67-77. [Content Brief]
[3]. Li YX, et al. Transportan Peptide Stimulates the Nanomaterial Internalization into Mammalian Cells in the Bystander Manner through Macropinocytosis. Pharmaceutics. 2021;13(4):552. Published 2021 Apr 14. [Content Brief]
[4]. Li YX, et al. Co-administration of Transportan Peptide Enhances the Cellular Entry of Liposomes in the Bystander Manner Both In Vitro and In Vivo. Mol Pharm. 2022;19(11):4123-4134. [Content Brief]
[5]. Lindgren ME, et al. Passage of cell-penetrating peptides across a human epithelial cell layer in vitro. Biochem J. 2004;377(Pt 1):69-76. [Content Brief]
[6]. Pepe D, et al. Transportan in nanocarriers improves skin localization and antitumor activity of paclitaxel. Int J Nanomedicine. 2016;11:2009-2019. Published 2016 May 11. [Content Brief]
[7]. Chugh A, et al. Cellular uptake of cell-penetrating peptides pVEC and transportan in plants. J Pept Sci. 2008;14(4):477-481. [Content Brief]
[8]. Zhang C, et al. Transportan-derived cell-penetrating peptide delivers siRNA to inhibit replication of influenza virus in vivo. Drug Des Devel Ther. 2019;13:1059-1068. Published 2019 Apr 4. [Content Brief]
[9]. Izabela R, et al. Transportan 10 improves the anticancer activity of cisplatin. Naunyn Schmiedebergs Arch Pharmacol. 2016;389(5):485-497. [Content Brief]
[10]. Pooga M, et al. Cell penetrating PNA constructs regulate galanin receptor levels and modify pain transmission in vivo. Nat Biotechnol. 1998;16(9):857-861. [Content Brief]
[11]. Kaushik N, et al. Anti-TAR polyamide nucleotide analog conjugated with a membrane-permeating peptide inhibits human immunodeficiency virus type 1 production. J Virol. 2002;76(8):3881-3891. [Content Brief]
[12]. Basheer M, et al. Blood pressure modulation following activation of mast cells by cationic cell penetrating peptides. Peptides. 2011;32(12):2444-2451. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.3521 mL | 1.7603 mL | 3.5206 mL | 8.8014 mL |
| 5 mM | 0.0704 mL | 0.3521 mL | 0.7041 mL | 1.7603 mL | |
| 10 mM | 0.0352 mL | 0.1760 mL | 0.3521 mL | 0.8801 mL | |
| 15 mM | 0.0235 mL | 0.1174 mL | 0.2347 mL | 0.5868 mL | |
| 20 mM | 0.0176 mL | 0.0880 mL | 0.1760 mL | 0.4401 mL | |
| 25 mM | 0.0141 mL | 0.0704 mL | 0.1408 mL | 0.3521 mL | |
| 30 mM | 0.0117 mL | 0.0587 mL | 0.1174 mL | 0.2934 mL |