GHRH analog

Sermorelin binds to the growth hormone releasing hormone receptor and mimics native GRF in its ability to stimulate growth hormone secretion.

Sermorelin is used in the treatment of children with growth hormone deficiency or growth failure. Geref increases plasma growth hormone (GH) concentration by stimulating the pituitary gland to release GH. Geref is similar to the full-length native hormone (44 residues) in its ability to stimulate GH secretion in humans.

Biological half-life: 11-12 minutes

Depending on state or federal labeling requirements, termorelin acetate may cause developmental toxicity.

[1]. Drug Test Anal. 2016 Mar;8(3-4):398-401.

Sermorelin acetate may cause developmental toxicity depending on state or federal labeling requirements. Sermorelin is the bioactive fragment of human growth hormone releasing factor, consisting of a GHRH(1-29)-amide. This N-terminal sequence is identical in many mammals, such as humans, pigs, and cattle. It is used to diagnose or treat patients with growth hormone deficiency. See also: Sermorelin acetate (note moved here). Sermorelin is a 29-amino acid peptide used to treat growth problems caused by growth hormone deficiency (commonly occurring in children). It is the bioactive fragment of human growth hormone releasing factor (GHRH). It is used as a diagnostic reagent. It is a polypeptide and peptide hormone. Sermorelin acetate is an amidated acetate of a synthetic 29-amino acid peptide (GRF 1-29 NH 2 ), corresponding to the N-terminal fragment of naturally occurring human growth hormone releasing hormone (GHRH or GRF), which consists of 44 amino acid residues. It is the bioactive fragment of human growth hormone-releasing factor, composed of GHRH(1-29)-amide. This N-terminal sequence is identical in many mammals, such as humans, pigs, and cattle. It is used to diagnose or treat patients with growth hormone deficiency. See also: Semolorelin (note moved to).

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Drug Indications
For the treatment of dwarfism, prevention of HIV-induced weight loss
Mechanism of Action
Semolorelin binds to the growth hormone-releasing hormone receptor, and its ability to stimulate growth hormone secretion is similar to that of natural growth hormone-releasing hormone.
Pharmacodynamics
Semolorelin is used to treat growth hormone deficiency or growth retardation in children. Glifos increases plasma growth hormone concentration by stimulating the pituitary gland to release growth hormone (GH). Glifos is similar to the full-length natural hormone (44 amino acid residues) in stimulating the secretion of growth hormone in the human body. "Operation Pangoal" is an annual international action week to combat drug crime. In this study, entitled “Operation Resistance,” we asked institutions in European countries to search for counterfeit antibiotics and injectable biopeptides (peptides and proteins) among medicines seized during Operation Pangoal 7 (2014). Belgium, Cyprus, Czech Republic, Denmark, France, Netherlands, Portugal, Sweden, Spain, United Kingdom, Norway, and Switzerland all reported findings. These countries reported seizures of approximately 21,000 doses (e.g., tablets, capsules) of counterfeit antibiotics. The majority of these were commonly used antibiotics without proper authorization. This week, the number of counterfeit injectable biopharmaceuticals reported was extremely small. Counterfeit products reported by laboratories included human growth hormone, sermorepinephrine, melanostatin II, and products without any active ingredients. The average shipment volume appears excessively large and not intended for personal use, suggesting a significant portion of these products are intended for resale. This study outlines the situation of counterfeit antibiotics and biopharmaceuticals entering European countries. It remains unclear how many counterfeit products ultimately reached consumers during Operation Pan-Continental and other weeks. The shipment volumes indicate that the importation of counterfeit antibiotics and biopharmaceuticals is for both personal use and resale. The use of antibiotics of unknown origin can harm health, exacerbate antibiotic resistance, and make it difficult for health authorities to identify sources of infection. Counterfeit biopharmaceuticals also pose health risks because they lack all labeling and may contain unlicensed injectable drugs. Raising awareness among healthcare professionals is crucial, as counterfeit drugs in Europe are not limited to medications for treating erectile dysfunction. [1]

C151H250N44O44S

3417.93413305283

3355.82

C, 53.06; H, 7.37; N, 18.03; O, 20.60; S, 0.94

114466-38-5

114466-38-5 (acetate); 86168-78-7;

16132412

H-Tyr-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyr-Arg-Lys-Val-Leu-Gly-Gln-Leu-Ser-Ala-Arg-Lys-Leu-Leu-Gln-Asp-Ile-Met-Ser-Arg-NH2.CH3CO2H; L-tyrosyl-L-alanyl-L-alpha-aspartyl-L-alanyl-L-isoleucyl-L-phenylalanyl-L-threonyl-L-asparagyl-L-seryl-L-tyrosyl-L-arginyl-L-lysyl-L-valyl-L-leucyl-glycyl-L-glutaminyl-L-leucyl-L-seryl-L-alanyl-L-arginyl-L-lysyl-L-leucyl-L-leucyl-L-glutaminyl-L-alpha-aspartyl-L-isoleucyl-L-methionyl-L-seryl-L-argininamide acetic acid

YADAIFTNSYRKVLGQLSARKLLQDIMSR

Typically exists as solid at room temperature

5.07

53

51

118

240

7670

31

S(C)CC[C@@H](C(N[C@H](C(N[C@H](C(N)=O)CCCNC(=N)N)=O)CO)=O)NC([C@H]([C@@H](C)CC)NC([C@H](CC(=O)O)NC([C@H](CCC(N)=O)NC([C@H](CC(C)C)NC([C@H](CC(C)C)NC([C@H](CCCCN)NC([C@H](CCCNC(=N)N)NC([C@H](C)NC([C@H](CO)NC([C@H](CC(C)C)NC([C@H](CCC(N)=O)NC(CNC([C@H](CC(C)C)NC([C@H](C(C)C)NC([C@H](CCCCN)NC([C@H](CCCNC(=N)N)NC([C@H](CC1C=CC(=CC=1)O)NC([C@H](CO)NC([C@H](CC(N)=O)NC([C@H]([C@@H](C)O)NC([C@H](CC1C=CC=CC=1)NC([C@H]([C@@H](C)CC)NC([C@H](C)NC([C@H](CC(=O)O)NC([C@H](C)NC([C@H](CC1C=CC(=CC=1)O)N)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O.OC(C)=O

BVLCEKWPOSAKSZ-YQMCHIOTSA-N

InChI=1S/C149H246N44O42S.C2H4O2/c1-20-77(13)116(191-122(211)81(17)168-132(221)104(66-113(204)205)178-121(210)79(15)167-123(212)88(152)62-84-39-43-86(198)44-40-84)145(234)185-102(63-83-32-23-22-24-33-83)138(227)193-118(82(18)197)146(235)186-103(65-111(155)202)137(226)189-108(71-196)142(231)182-101(64-85-41-45-87(199)46-42-85)136(225)175-93(38-31-56-165-149(161)162)126(215)174-91(35-26-28-53-151)131(220)190-115(76(11)12)143(232)184-97(58-72(3)4)124(213)166-68-112(203)170-94(47-49-109(153)200)128(217)180-100(61-75(9)10)135(224)188-106(69-194)140(229)169-80(16)120(209)172-92(37-30-55-164-148(159)160)125(214)173-90(34-25-27-52-150)127(216)179-99(60-74(7)8)134(223)181-98(59-73(5)6)133(222)176-95(48-50-110(154)201)129(218)183-105(67-114(206)207)139(228)192-117(78(14)21-2)144(233)177-96(51-57-236-19)130(219)187-107(70-195)141(230)171-89(119(156)208)36-29-54-163-147(157)158;1-2(3)4/h22-24,32-33,39-46,72-82,88-108,115-118,194-199H,20-21,25-31,34-38,47-71,150-152H2,1-19H3,(H2,153,200)(H2,154,201)(H2,155,202)(H2,156,208)(H,166,213)(H,167,212)(H,168,221)(H,169,229)(H,170,203)(H,171,230)(H,172,209)(H,173,214)(H,174,215)(H,175,225)(H,176,222)(H,177,233)(H,178,210)(H,179,216)(H,180,217)(H,181,223)(H,182,231)(H,183,218)(H,184,232)(H,185,234)(H,186,235)(H,187,219)(H,188,224)(H,189,226)(H,190,220)(H,191,211)(H,192,228)(H,193,227)(H,204,205)(H,206,207)(H4,157,158,163)(H4,159,160,164)(H4,161,162,165);1H3,(H,3,4)/t77-,78-,79-,80-,81-,82+,88-,89-,90-,91-,92-,93-,94-,95-,96-,97-,98-,99-,100-,101-,102-,103-,104-,105-,106-,107-,108-,115-,116-,117-,118-;/m0./s1

H-Tyr-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyr-Arg-Lys-Val-Leu-Gly-Gln-Leu-Ser-Ala-Arg-Lys-Leu-Leu-Gln-Asp-Ile-Met-Ser-Arg-NH2

GHRH (1-29); Sermorelin acetate; trade name: Geref.

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

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

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.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*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).

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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)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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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).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)