83103-21-3

Upstream product

• 2188-18-3 Boc-Arg(NO₂)-OH 
• 1738-68-7 Gly-OBz 
• 1738-76-7 glycine benzyl ester p-toluenesulfonic acid salt 
• 63366-76-7 (toluene-4-sulfonylamino)acetic acid benzyl ester 

Downstream Products

• 1148136-92-8 C₃₂H₅₁N₇O₁₀ 
• 1148136-95-1 C₃₄H₅₅N₇O₁₀ 
• 1148136-98-4 C₃₆H₅₉N₇O₁₀ 
• 1148137-03-4 C₃₈H₆₃N₇O₁₀ 
• 1148137-07-8 C₄₀H₆₇N₇O₁₀ 
• 1148137-11-4 C₄₂H₇₁N₇O₁₀ 
• 246516-47-2 Boc-Arg(Nω-NO2)-Gly-Asp(OBn)-Ser(Bn)-OBn 
• 350688-05-0 Boc-Arg(Nω-NO2)-Gly-Asp(OBn)-Val-OBn 
• 93674-99-8 RGDV 
• 906673-81-2 Boc-Arg(Nω-NO2)-Gly-Asp(OBn)-Phe-OBn 
• 110697-46-6 H-Arg-Gly-Asp-Phe-OH 
• 186379-70-4 Arg(NO₂)-Gly-Asp(OBzl)-OBzl 
• 1223438-41-2 C₄₂H₆₃N₇O₉ 
• 1223438-39-8 C₄₀H₅₉N₇O₉ 

Relevant academic research and scientific papers

RGDV-modified gemcitabine: A nano-medicine capable of prolonging half-life, overcoming resistance and eliminating bone marrow toxicity of gemcitabine

Background: Gemcitabine has been widely used as a chemotherapeutic drug. However, drug resistance, short half-life and side effects seriously decrease its chemotherapeutic efficacy. Purpose: The object of preparing RGDV-gemcitabine was to prolong the half

Design and synthesis of nanoscaled IQCA-TAVV as a delivery system capable of antiplatelet activation, targeting arterial thrombus and releasing IQCA

Background: Arterial thrombosis has been associated with a series of pathological conditions, and the discovery of arterial thrombosis inhibitor is of clinical importance. Methods: By analyzing the pharmacophores of anti-platelet agents, thrombus targeting peptide and anti-thrombotic nano-systems 3S-1,2,3,4-tetrahydroisoquino- line-3-carbonyl-Thr-Ala- Arg-Gly-Asp(Val)-Val (IQCA-TAVV) was designed and prepared as a nano-scaled arterial thrombosis inhibitor. Results: In vitro the nanoparticles of IQCA-TAVV were able to adhere onto the surface of activated platelets, attenuate activated platelets to extend pseudopodia and inhibit activated platelets to form aggregators. In vivo IQCA-TAVV targeted arterial thrombus, dose depend- ently inhibited arterial thrombosis with a 1 nmol/kg of minimal effective dose, and the activity was ~1670 folds of that of aspirin. Conclusion: IQCA-TAVV represented the design, preparation and application of nanomedicine capable of adhering on the surface of activated platelets, attenuating platelet activation, targeting arterial thrombus and inhibiting arterial thrombosis.

IQCA-TASS: a nano-scaled P-selectin inhibitor capable of targeting thrombus and releasing IQCA/TARGD(S)S in vivo

Thrombosis is a serious threat to human health worldwide. Tetrahydroisoquinoline-3-carboxylic acid (IQCA) is an antithrombotic agent, while Thr-Ala-Arg-Gly-Asp(Ser)-Ser (TASS) can target thrombus. Herein, tetrahydro-isoquinoline-3-carbonyl-Thr-Ala-Arg-Gly-Asp(Ser)-Ser (IQCA-TASS) was designed with the aim towards the discovery of a nano-delivery system for targeting thrombus. In vitro, IQCA-TASS acted on P-selectin and down-regulated P-selectin expression. The IC50 values of IQCA-TASS against the platelet aggregation induced by four aggregators were less than 0.45 nM. In vivo, IQCA-TASS targeted thrombus, released IQCA and TASS inside the thrombus, showed dose-dependent anti-thrombotic action, of which the minimal effective dose was 1 nmol kg-1, and showed anti-inflammatory action. Even with the dose up to 1 μmol kg-1, a dose of 1000 times the minimal effective dose, IQCA-TASS still induced no toxic reaction. In rat plasma, IQCA-TASS formed nanoparticles with diameters of less than 41 nm. The interactions of the nanoparticles with both resting and activated platelets were imaged. IQCA-TASS should be a safe nano-medicine capable of targeting thrombus and releasing anti-thrombotic/anti-inflammatory pharmacophores in disease sites.

RGD-peptides modifying dexamethasone: to enhance the anti-inflammatory efficacy and limit the risk of osteoporosis

Dexamethasone (Dex) is one of the most effective anti-inflammatory glucocorticoids, while the side effect, osteoporosis seriously limits its clinical use. Cell adhesion is involved in the onset of inflammation and osteoporosis, and RGD-peptides are well k

RGD-fatty alcohol-modified docetaxel liposomes improve tumor selectivity in vivo

The tripeptide arginine-glycine-aspartate (RGD) was conjugated with various fatty alcohols to obtain RGDOCnH2n + 1 (n = 8, 10, 12, 14, 16, 18), which were incorporated into the bilayer of docetaxel liposomes to improve their tumor sp

Preparation and biological evaluation of tumor-specific Ara-C liposomal preparations containing RGDV motif

Arginine-glycine-aspartate (RGD) has been shown to be essential for the recognition of integrins overexpressed in tumor cells, especially during tumor invasion, angiogenesis, and metasis. In this study, a novel tetrapeptide, RGD-valine (RGDV), was designe

Novel tetrapeptide, RGDF, mediated tumor specific liposomal doxorubicin (DOX) preparations

Arginine-glycine-aspartate (RGD) has been shown to possess a strong affinity for the integrins overexpressed in tumor cells, especially during tumor invasion, angiogenesis and metasis. Based on work from others, a novel tetrapeptide, arginine-glycine-aspa

Deblocking of peptides with proton donors

A series of model di- and tripeptides were synthesized, and they were deblocked with ammonium formate and cyclohexene in the presence of a palladium catalyst.It was shown that the deblocking of the peptides containing nitroarginine takes place readily and

Studies of Bitter Peptides from Casein Hydrolyzate. VIII. Bitter Taste of Cyclic Analog of BPIa (Arg-Gly-Pro-Pro-Phe-Ile-Val)

In order to elucidate the structure-taste relationship of bitter peptide BPIa (Arg-Gly-Pro-Pro-Phe-Ile-Val), cyclo-BPIa was synthesized.The result of both taste and CD examinations suggested that the bitterness of BPIa is caused by its spatial structure,