| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 1g | |||
| Other Sizes |
| Targets |
Secretin receptor (a G-protein-coupled receptor). Activation stimulates the adenylate cyclase (AC)/protein kinase A (PKA) pathway and increases intracellular Ca²⁺ concentration. Rat and human secretin receptors share 81% identity. Vasoactive intestinal peptide (VIP) binds to secretin receptors with an affinity similar to secretin. [1]
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| ln Vitro |
Rats' release of adrenocorticotropic hormone (ACTH) is inhibited by secretin (33-59), which also specifically blocks the glucocorticoid response to ACTH in zona fasciculata reticularis (ZF/R) cells [1]. In the rat cerebellum, the secretin retrograde messenger facilitates GABA transmission [2].
Secretin (at 10⁻⁷ M) maximally enhanced aldosterone production (2.4-fold increase) by dispersed rat zona glomerulosa (ZG) cells. [1] Secretin did not affect basal corticosterone production by dispersed rat zona fasciculata/reticularis (ZF/R) cells. [1] Secretin inhibited both submaximally (10⁻¹⁰ M ACTH) and maximally (10⁻⁸ M ACTH) stimulated corticosterone secretion from dispersed rat ZF/R cells. [1] Secretin did not stimulate corticosterone secretion in cultured murine adrenal tumor cells. [1] Secretin enhanced catecholamine synthesis in rat PC12 pheochromocytoma cells. [1] |
| ln Vivo |
In rats, a single subcutaneous (SC) bolus of Secretin (30 nmol/kg) moderately attenuated the injection stress-induced rise in plasma ACTH at 60 min, but significantly increased ACTH levels above control at 120 min. [1]
Prolonged SC administration of Secretin (10 or 30 nmol/kg/day for 6 days) markedly elevated basal blood ACTH concentration in rats. [1] A single SC bolus of Secretin (30 nmol/kg) increased plasma aldosterone levels at 120 min in rats. [1] Chronic treatment with Secretin (10 or 30 nmol/kg/day for 6 days) stably elevated basal plasma aldosterone in rats. [1] A single SC injection of Secretin (30 nmol/kg) caused a 60% suppression of the stress-induced corticosterone rise at 60 min, followed by a rebound increase above control at 120 min in rats. [1] Chronic Secretin treatment (10 or 30 nmol/kg/day for 6 days) increased basal plasma corticosterone and adrenal gland weight in rats. [1] One study reported no change in rat plasma corticosterone 60 min after an intraperitoneal (IP) bolus of Secretin (dose unspecified). [1] |
| Cell Assay |
Steroidogenic effects were assessed using dispersed adrenocortical cells. Rat adrenal glands were decapsulated to isolate the zona glomerulosa (ZG). The remaining tissue (zona fasciculata/reticularis, ZF/R) was processed separately. Tissues were minced and digested with collagenase to obtain dispersed cells. Cells were incubated in appropriate culture medium. Aldosterone production was measured in ZG cell incubations. Corticosterone production, both basal and in response to ACTH stimulation, was measured in ZF/R cell incubations. Steroid hormone concentrations in the incubation media were quantified by radioimmunoassay. [1]
The effect on catecholamine synthesis was studied using the rat PC12 pheochromocytoma cell line. [1] |
| Animal Protocol |
Acute Study: Rats received a single subcutaneous (SC) bolus injection of Secretin at a dose of 30 nmol/kg. Blood samples were collected at 60 and 120 minutes post-injection for the measurement of plasma ACTH, aldosterone, and corticosterone levels. The injection procedure itself served as a mild stressor. [1]
Chronic Study: Rats were treated with Secretin via daily subcutaneous (SC) injection for 6 consecutive days at doses of 10 or 30 nmol/kg per day. Following the treatment period, animals were euthanized, and blood was collected to determine basal hormone concentrations. Adrenal glands were excised and weighed. [1] In a separate experiment, Secretin was administered as a single intraperitoneal (IP) bolus injection, and plasma corticosterone was measured 60 minutes later. [1] |
| References | |
| Additional Infomation |
Secretin is a 27-amino acid peptide belonging to the vasoactive intestinal peptide (VIP)-secretin-glucagon family. It is expressed in the hypothalamus and pituitary gland. Its receptors are also present in these brain regions, but the evidence for the presence of receptors in the adrenal glands is based on indirect evidence from functional studies. [1] Secretin regulates the hypothalamic-pituitary-adrenal (HPA) axis through a complex mechanism. It can stimulate the release of adrenocorticotropic hormone (ACTH), which may be achieved by activating hypothalamic receptors and CRH-releasing hormone (CRH) neurons. It directly stimulates the secretion of aldosterone by zona glomerulosa (ZG) cells, but inhibits the production of glucocorticoids by ZF/R cells stimulated by ACTH. The peptide may also indirectly affect adrenal function by regulating adrenal blood flow or medullary chromaffin cell activity. [1] Food intake-induced physiological secretin secretion may be associated with increased adrenal steroid secretion related to food intake. [1]
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| Molecular Formula |
C129H216N42O42
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|---|---|
| Molecular Weight |
3027.35153999999
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| Exact Mass |
3025.61
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| CAS # |
121028-49-7
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| Related CAS # |
Secretin (33-59), rat TFA
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| PubChem CID |
90488725
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.505 g/cm3
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| LogP |
-14.4
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| Hydrogen Bond Donor Count |
50
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| Hydrogen Bond Acceptor Count |
47
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| Rotatable Bond Count |
107
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| Heavy Atom Count |
213
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| Complexity |
6940
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| Defined Atom Stereocenter Count |
27
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| SMILES |
OCCC(NCC(NCC(NCC(NCC(NCC(NCC(NCC(NCC(NCC(NCC(NCC(NCC(NCC(NCC(NCC(NCC=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O
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| InChi Key |
LKHWQEXKRMDFFJ-NEMWHCQRSA-N
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| InChi Code |
InChI=1S/C129H216N42O42/c1-58(2)40-78(119(206)170-99(64(13)14)102(134)189)149-94(181)51-145-105(192)74(29-33-91(131)178)153-113(200)81(43-61(7)8)161-116(203)82(44-62(9)10)159-108(195)72(27-22-38-143-128(137)138)151-110(197)75(30-34-92(132)179)154-114(201)79(41-59(3)4)157-107(194)71(26-21-37-142-127(135)136)150-103(190)65(15)148-121(208)87(53-172)166-118(205)86(49-98(187)188)163-111(198)76(31-35-93(133)180)155-115(202)80(42-60(5)6)158-109(196)73(28-23-39-144-129(139)140)152-122(209)89(55-174)167-117(204)83(45-63(11)12)160-112(199)77(32-36-96(183)184)156-123(210)90(56-175)168-126(213)101(67(17)177)171-120(207)84(46-68-24-19-18-20-25-68)164-125(212)100(66(16)176)169-95(182)52-146-106(193)85(48-97(185)186)162-124(211)88(54-173)165-104(191)70(130)47-69-50-141-57-147-69/h18-20,24-25,50,57-67,70-90,99-101,172-177H,21-23,26-49,51-56,130H2,1-17H3,(H2,131,178)(H2,132,179)(H2,133,180)(H2,134,189)(H,141,147)(H,145,192)(H,146,193)(H,148,208)(H,149,181)(H,150,190)(H,151,197)(H,152,209)(H,153,200)(H,154,201)(H,155,202)(H,156,210)(H,157,194)(H,158,196)(H,159,195)(H,160,199)(H,161,203)(H,162,211)(H,163,198)(H,164,212)(H,165,191)(H,166,205)(H,167,204)(H,168,213)(H,169,182)(H,170,206)(H,171,207)(H,183,184)(H,185,186)(H,187,188)(H4,135,136,142)(H4,137,138,143)(H4,139,140,144)/t65-,66+,67+,70-,71-,72-,73-,74-,75-,76-,77-,78-,79-,80-,81-,82-,83-,84-,85-,86-,87-,88-,89-,90-,99-,100-,101-/m0/s1
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| Chemical Name |
(4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[2-[[(2S)-1-[[(2S)-1-amino-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-5-oxopentanoic acid
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 0.3303 mL | 1.6516 mL | 3.3032 mL | |
| 5 mM | 0.0661 mL | 0.3303 mL | 0.6606 mL | |
| 10 mM | 0.0330 mL | 0.1652 mL | 0.3303 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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