Yoda1
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MedKoo CAT#: 562426

CAS#: 448947-81-7

Description: Yoda1, also known as GlyT2-IN-1, is an agonist of the mechanotransduction channel Piezo1. It acts by eliciting Ca2+ flux in Piezo1- but not vector-transfected cells.


Chemical Structure

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Yoda1
CAS# 448947-81-7

Theoretical Analysis

MedKoo Cat#: 562426
Name: Yoda1
CAS#: 448947-81-7
Chemical Formula: C13H8Cl2N4S2
Exact Mass: 353.9567
Molecular Weight: 355.25
Elemental Analysis: C, 43.95; H, 2.27; Cl, 19.96; N, 15.77; S, 18.05

Price and Availability

Size Price Availability Quantity
5.0mg USD 90.0 Ready to ship
10.0mg USD 150.0 Ready to ship
25.0mg USD 250.0 Ready to ship
50.0mg USD 450.0 Ready to ship
100.0mg USD 750.0 Ready to ship
200.0mg USD 1250.0 Ready to ship
500.0mg USD 2650.0 Ready to ship
1.0g USD 3850.0 Ready to ship
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Related CAS #: 448947-81-7  

Synonym: Yoda1; Yoda-1; Yoda 1; GlyT2-IN-1; GlyT2-IN 1; GlyT2-IN1;

IUPAC/Chemical Name: 2-[5-(2,6-Dichloro-benzylsulfanyl)-[1,3,4]thiadiazol-2-yl]-pyrazine

InChi Key: BQNXBSYSQXSXPT-UHFFFAOYSA-N

InChi Code: InChI=1S/C13H8Cl2N4S2/c14-9-2-1-3-10(15)8(9)7-20-13-19-18-12(21-13)11-6-16-4-5-17-11/h1-6H,7H2

SMILES Code: ClC1=C(C(Cl)=CC=C1)CSC2=NN=C(C3=NC=CN=C3)S2

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Biological target: Yoda 1 is a Piezo1 agonist.
In vitro activity: Yoda1 incubation weakly induced phosphorylation of p38 for at least 60 min, which was less clear for orbital shaking (Figure 2A). Phosphorylation of ERK was more prominent. Orbital shaking induced ERK phosphorylation for 60 min, whereas Yoda1 incubation induced transient ERK phosphorylation with a peak at 10 min. JNK was not phosphorylated by orbital shaking, whereas Yoda1 incubation induced JNK phosphorylation reaching a maximum at 60 min (Figure 2C). Reference: Int J Mol Sci. 2021 Jan; 22(2): 955. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7835781/
In vivo activity: Findings demonstrated that Yoda1-induced intracellular calcium increases in mouse DRG neurons and Yoda1-induced intracellular Ca2+ increases disappear in the absence of extracellular Ca2+. This suggests that these Ca2+ increases are caused via activation of ion channel in plasma membranes, but not organelles in cells. These Ca2+ responses were inhibited by ruthenium red and GsMTx4, indicating that the channel, which was activated by Yoda1, is a mechanosensitive cation channel. However, the other mechanosensitive ion channel, TRPV4, is known to be in DRG neurons. In MC353-E1 cells, TRPV4-knockdown blocked Yoda1-induced Ca2+ response as well as GSK1016790A, a TRPV4 agonist. Yoda1-induced Ca2+ response can be either in TRPV4-dependent or independent manners. When both Piezo1 and TRPV4 were highly expressed, Yoda1 induced a TRPV4-dependent Ca2+ response via activation of Piezo1. Reference: Int J Mol Sci. 2020 Jun; 21(11): 3834. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7313462/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 11.15 31.39
DMF 5.0 14.07
DMF:PBS (pH 7.2) (1:2) 0.3 0.84

Preparing Stock Solutions

The following data is based on the product molecular weight 355.25 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Aglialoro F, Abay A, Yagci N, Rab MAE, Kaestner L, van Wijk R, von Lindern M, van den Akker E. Mechanical Stress Induces Ca2+-Dependent Signal Transduction in Erythroblasts and Modulates Erythropoiesis. Int J Mol Sci. 2021 Jan 19;22(2):955. doi: 10.3390/ijms22020955. PMID: 33478008; PMCID: PMC7835781. 2. Kuntze A, Goetsch O, Fels B, Najder K, Unger A, Wilhelmi M, Sargin S, Schimmelpfennig S, Neumann I, Schwab A, Pethő Z. Protonation of Piezo1 Impairs Cell-Matrix Interactions of Pancreatic Stellate Cells. Front Physiol. 2020 Feb 14;11:89. doi: 10.3389/fphys.2020.00089. PMID: 32116794; PMCID: PMC7033545. 3. Roh J, Hwang SM, Lee SH, Lee K, Kim YH, Park CK. Functional Expression of Piezo1 in Dorsal Root Ganglion (DRG) Neurons. Int J Mol Sci. 2020 May 28;21(11):3834. doi: 10.3390/ijms21113834. PMID: 32481599; PMCID: PMC7313462. 4. Wang J, La JH, Hamill OP. PIEZO1 Is Selectively Expressed in Small Diameter Mouse DRG Neurons Distinct From Neurons Strongly Expressing TRPV1. Front Mol Neurosci. 2019 Jul 19;12:178. doi: 10.3389/fnmol.2019.00178. PMID: 31379500; PMCID: PMC6659173.
In vitro protocol: 1. Aglialoro F, Abay A, Yagci N, Rab MAE, Kaestner L, van Wijk R, von Lindern M, van den Akker E. Mechanical Stress Induces Ca2+-Dependent Signal Transduction in Erythroblasts and Modulates Erythropoiesis. Int J Mol Sci. 2021 Jan 19;22(2):955. doi: 10.3390/ijms22020955. PMID: 33478008; PMCID: PMC7835781. 2. Kuntze A, Goetsch O, Fels B, Najder K, Unger A, Wilhelmi M, Sargin S, Schimmelpfennig S, Neumann I, Schwab A, Pethő Z. Protonation of Piezo1 Impairs Cell-Matrix Interactions of Pancreatic Stellate Cells. Front Physiol. 2020 Feb 14;11:89. doi: 10.3389/fphys.2020.00089. PMID: 32116794; PMCID: PMC7033545.
In vivo protocol: 1. Roh J, Hwang SM, Lee SH, Lee K, Kim YH, Park CK. Functional Expression of Piezo1 in Dorsal Root Ganglion (DRG) Neurons. Int J Mol Sci. 2020 May 28;21(11):3834. doi: 10.3390/ijms21113834. PMID: 32481599; PMCID: PMC7313462. 2. Wang J, La JH, Hamill OP. PIEZO1 Is Selectively Expressed in Small Diameter Mouse DRG Neurons Distinct From Neurons Strongly Expressing TRPV1. Front Mol Neurosci. 2019 Jul 19;12:178. doi: 10.3389/fnmol.2019.00178. PMID: 31379500; PMCID: PMC6659173.

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1: Evans EL, Cuthbertson K, Endesh N, Rode B, Blythe NM, Hyman AJ, Hall SJ, Gaunt HJ, Ludlow MJ, Foster R, Beech DJ. Yoda1 analogue (Dooku1) which antagonises Yoda1-evoked activation of Piezo1 and aortic relaxation. Br J Pharmacol. 2018 Mar 2. doi: 10.1111/bph.14188. [Epub ahead of print] PubMed PMID: 29498036.

2: Dela Paz NG, Frangos JA. Yoda1-induced phosphorylation of Akt and ERK1/2 does not require Piezo1 activation. Biochem Biophys Res Commun. 2018 Feb 26;497(1):220-225. doi: 10.1016/j.bbrc.2018.02.058. Epub 2018 Feb 8. PubMed PMID: 29428723; PubMed Central PMCID: PMC5835220.

3: Sugimoto A, Miyazaki A, Kawarabayashi K, Shono M, Akazawa Y, Hasegawa T, Ueda-Yamaguchi K, Kitamura T, Yoshizaki K, Fukumoto S, Iwamoto T. Piezo type mechanosensitive ion channel component 1 functions as a regulator of the cell fate determination of mesenchymal stem cells. Sci Rep. 2017 Dec 18;7(1):17696. doi: 10.1038/s41598-017-18089-0. PubMed PMID: 29255201; PubMed Central PMCID: PMC5735093.

4: Beech DJ. Endothelial Piezo1 channels as sensors of exercise. J Physiol. 2018 Mar 15;596(6):979-984. doi: 10.1113/JP274396. Epub 2018 Jan 9. PubMed PMID: 29194632; PubMed Central PMCID: PMC5851887.

5: Gnanasambandam R, Gottlieb PA, Sachs F. The Kinetics and the Permeation Properties of Piezo Channels. Curr Top Membr. 2017;79:275-307. doi: 10.1016/bs.ctm.2016.11.004. Epub 2017 Jan 11. Review. PubMed PMID: 28728821.

6: Ilkan Z, Wright JR, Goodall AH, Gibbins JM, Jones CI, Mahaut-Smith MP. Evidence for shear-mediated Ca(2+) entry through mechanosensitive cation channels in human platelets and a megakaryocytic cell line. J Biol Chem. 2017 Jun 2;292(22):9204-9217. doi: 10.1074/jbc.M116.766196. Epub 2017 Apr 17. PubMed PMID: 28416610; PubMed Central PMCID: PMC5454102.

7: Wang S, Chennupati R, Kaur H, Iring A, Wettschureck N, Offermanns S. Endothelial cation channel PIEZO1 controls blood pressure by mediating flow-induced ATP release. J Clin Invest. 2016 Dec 1;126(12):4527-4536. doi: 10.1172/JCI87343. Epub 2016 Oct 31. PubMed PMID: 27797339; PubMed Central PMCID: PMC5127677.

8: Syeda R, Xu J, Dubin AE, Coste B, Mathur J, Huynh T, Matzen J, Lao J, Tully DC, Engels IH, Petrassi HM, Schumacher AM, Montal M, Bandell M, Patapoutian A. Chemical activation of the mechanotransduction channel Piezo1. Elife. 2015 May 22;4. doi: 10.7554/eLife.07369. PubMed PMID: 26001275; PubMed Central PMCID: PMC4456433.

9: Cahalan SM, Lukacs V, Ranade SS, Chien S, Bandell M, Patapoutian A. Piezo1 links mechanical forces to red blood cell volume. Elife. 2015 May 22;4. doi: 10.7554/eLife.07370. PubMed PMID: 26001274; PubMed Central PMCID: PMC4456639.

Yoda1

5.0mg / USD 90.0