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TFLLR-NH2 (TFA)

Cat. No. M31168
TFLLR-NH2 (TFA) Structure
Size Price Availability Quantity
1mg USD 210  USD210 In stock
5mg USD 850  USD850 In stock
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Quality Control & Documentation
Biological Activity

TFLLR-NH2 (TFA) is a selective protease-activated receptor 1 (PAR1) agonist with an EC50 value of 1.9 μM.

Chemical Information
Molecular Weight 761.85
Formula C33H54F3N9O8
CAS Number 1313730-19-6
Form Solid
Storage -20°C
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Tomaz Alves, et al. Sci Rep. Osteogenesis in human periodontal ligament stem cell sheets is enhanced by the protease-activated receptor 1 (PAR1) in vivo

[2] Dong Hoon Shin, et al. Pharmacology. Regulation of the Pacemaker Activity of Colonic Interstitial Cells of Cajal by Protease-Activated Receptors: Involvement of Hyperpolarization-Activated Cyclic Nucleotide Channels

[3] Yitao Jia, et al. Oncol Rep. Activation of platelet protease-activated receptor-1 induces epithelial-mesenchymal transition and chemotaxis of colon cancer cell line SW620

[4] Shih-Che Huang. Regul Pept. Protease-activated receptor-1 (PAR1) and PAR2 but not PAR4 mediate relaxations in lower esophageal sphincter

[5] J W Fenton 2nd, et al. Curr Drug Targets Cardiovasc Haematol Disord. Statins and thrombin

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Keywords: TFLLR-NH2 (TFA) supplier, PAR, inhibitors, activators


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